Nampt inhibitors

ABSTRACT

Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.

This application claims priority to U.S. Provisional Application Ser.No. 61/645,679, filed May 11, 2012, U.S. Provisional Application Ser.No. 61/718,998, filed Oct. 26, 2012, and U.S. Provisional ApplicationSer. No. 61/779,626, filed Mar. 13, 2013, which are incorporated byreference in their entirety.

FIELD OF THE INVENTION

This invention pertains to compounds which inhibit the activity ofNAMPT, compositions containing the compounds, and methods of treatingdiseases during which NAMPT is expressed.

BACKGROUND OF THE INVENTION

NAD+ (nicotinamide adenine dinucleotide) is a coenzyme that plays acritical role in many physiologically essential processes (Ziegkel, M.Eur. J. Biochem. 267, 1550-1564, 2000). NAD is necessary for severalsignaling pathways including among others poly ADP-ribosylation in DNArepair, mono-ADP-ribosylation in both the immune system andG-protein-coupled signaling, and NAD is also required by sirtuins fortheir deacetylase activity (Garten, A. et al Trends in Endocrinology andMetabolism, 20, 130-138, 2008).

NAMPT (also known as pre-B-cell-colony-enhancing factor (PBEF) andvisfatin) is an enzyme that catalyzes the phosphoribosylation ofnicotinamide and is the rate-limiting enzyme in one of two pathways thatsalvage NAD.

Increasing evidence suggests that NAMPT inhibitors have potential asanticancer agents. Cancer cells have a higher basal turnover of NAD andalso display higher energy requirements compared with normal cells.Additionally, increased NAMPT expression has been reported in colorectalcancer (Van Beijnum, J. R. et al Int. J. Cancer 101, 118-127, 2002) andNAMPT is involved in angiogenesis (Kim, S. R. et al. Biochem. Biophys.Res. Commun. 357, 150-156, 2007). Small-molecule inhibitors of NAMPThave been shown to cause depletion of intracellular NAD+ levels andultimately induce tumor cell death (Hansen, C M et al. Anticancer Res.20, 42111-4220, 2000) as well as inhibit tumor growth in xenograftmodels (Olese, U. H. et al. Mol Cancer Ther. 9, 1609-1617, 2010).

NAMPT inhibitors also have potential as therapeutic agents ininflammatory and metabolic disorders (Galli, M. et al Cancer Res. 70,8-11, 2010). For example, NAMPT is the predominant enzyme in T and Blymphocytes. Selective inhibition of NAMPT leads to NAD+ depletion inlymphocytes blocking the expansion that accompanies autoimmune diseaseprogression whereas cell types expressing the other NAD+ generatingpathways might be spared. A small molecule NAMPT inhibitor (FK866) hasbeen shown to selectively block proliferation and induce apoptosis ofactivated T cells and was efficacious in animal models of arthritis(collagen-induced arthritis) (Busso, N. et al. Plos One 3, e2267, 2008).FK866 ameliorated the manifestations of experimental autoimmuneencephalomyelitis (EAE), a model of T-cell mediated autoimmunedisorders. (Bruzzone, S et al. Plos One 4, e7897, 2009). NaMPT activityincreases NF-kB transcriptional activity in human vascular endothelialcell, resulting in MMP-2 and MMP-9 activation, suggesting a role forNAMPT inhibitors in the prevention of inflammatory mediatedcomplications of obesity and type 2 diabetes (Adya, R. et. Al. DiabetesCare, 31, 758-760, 2008).

SUMMARY OF THE INVENTION

One embodiment, therefore, pertains to compounds or pharmaceuticallyacceptable salts thereof, which are useful as inhibitors of NAMPT, thecompounds having Formula (IB)

or a therapeutically acceptable salt thereof, wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

Z is CH, C—F, C—Cl, C—Br, C—I or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is hydrogen, F, Cl, Br, or I;

Z is CR²; and

R² is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R^(3x) is independently selected from the group consisting of phenyl andheterocyclyl; wherein each R^(3x) phenyl and heterocyclyl is substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴,OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂,NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH,C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I;

R¹¹ at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

m is 4, 5, or 6; and

n is 1 or 2;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is hydrogen; and R³is phenyl; the R³ phenyl is not substituted at the para position withphenyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

In another embodiment of Formula (IB), R¹ is NHC(O)NHR³; and R² ishydrogen. In another embodiment of Formula (IB), R¹ is CH₂NHC(O)R³; andR² is hydrogen. In another embodiment of Formula (IB), R¹ is hydrogen;and R² is CH₂NHC(O)NHR³. In another embodiment of Formula (IB), R¹ ishydrogen; and R² is CH₂NHC(O)R³. In one embodiment of Formula (IB), R³is phenyl; wherein each R³ phenyl is substituted at the para positionwith one substituent independently selected from the group consisting ofR⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, andC(O)NHR⁴; and wherein each R³ phenyl is optionally additionallysubstituted with one substituent independently selected from the groupconsisting of F, Cl, Br and I. In one embodiment of Formula (IB), R¹ isNHC(O)NHR³; R² is hydrogen; and R³ is phenyl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inone embodiment of Formula (IB), R¹ is CH₂NHC(O)R³; R² is hydrogen; andR³ is phenyl; wherein each R³ phenyl is substituted at the para positionwith one substituent independently selected from the group consisting ofR⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, andC(O)NHR⁴; and wherein each R³ phenyl is optionally additionallysubstituted with one substituent independently selected from the groupconsisting of F, Cl, Br and I. In one embodiment of Formula (IB), R¹ ishydrogen; R² is CH₂NHC(O)NHR³; and R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inone embodiment of Formula (IB), R¹ is hydrogen; R² is CH₂NHC(O)R³; andR³ is phenyl; wherein each R³ phenyl is substituted at the para positionwith one substituent independently selected from the group consisting ofR⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, andC(O)NHR⁴; and wherein each R³ phenyl is optionally additionallysubstituted with one substituent independently selected from the groupconsisting of F, Cl, Br and I. In another embodiment of Formula (IB), R³is thienyl; wherein each R³ thienyl is substituted with one, two, orthree substituents independently selected from the group consisting ofR⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴,F, Cl, Br and I. In another embodiment of Formula (IB), R¹ isNHC(O)NHR³; R² is hydrogen; and R³ is thienyl; wherein each R³ thienylis substituted with one, two, or three substituents independentlyselected from the group consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In anotherembodiment of Formula (IB), R¹ is CH₂NHC(O)R³; R² is hydrogen; and R³ isthienyl; wherein each R³ thienyl is substituted with one, two, or threesubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I. In another embodiment of Formula (IB), R¹ is hydrogen; R²is CH₂NHC(O)NHR³; and R³ is thienyl; wherein each R³ thienyl issubstituted with one, two, or three substituents independently selectedfrom the group consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴,NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodimentof Formula (IB), R¹ is hydrogen; R² is CH₂NHC(O)R³; and R³ is thienyl;wherein each R³ thienyl is substituted with one, two, or threesubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

Still another embodiment pertains to compounds, which are

-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-7-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenylethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(morpholin-4-yl)ethyl]benzamide;-   N-(1-hydroxy-2-methylpropan-2-yl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-benzyl-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-(cyclopentylmethyl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(piperidin-1-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenoxyethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(pyrrolidin-1-yl)ethyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(propan-2-yloxy)ethyl]benzamide;-   N-(2-hydroxy-2-methylpropyl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-[2-hydroxy-1-(4-methoxyphenyl)ethyl]-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(2-oxopyrrolidin-1-yl)ethyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydrofuran-2-ylmethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-propylbenzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(morpholin-4-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-phenylbenzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-methylbutyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(2-oxopyrrolidin-1-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydro-2H-pyran-4-ylmethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide;-   N-[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(tetrahydrofuran-3-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)urea;-   1-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   2-ethoxy-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(morpholin-4-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(2-methoxyethoxy)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3-methoxy-2-methylpropanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}butanamide;-   4,4,4-trifluoro-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}butanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}tetrahydro-2H-pyran-4-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-4-methylpentanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-1-methylpiperidine-4-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}tetrahydro-2H-thiopyran-4-carboxamide    1,1-dioxide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-1,4-dioxane-2-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]butyl}piperidine-1-carboxylate;-   4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)benzamide;-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]butyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}urea;-   1-{4-[1-(cyclopentylcarbonyl)piperidin-4-yl]butyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]butyl}urea;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   2-cyclopentyl-N-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}acetamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(morpholin-4-ylacetyl)amino]benzamide;-   4-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate;-   N-{4-[(cyclopentylacetyl)amino]benzyl}imidazo[1,2-a]pyridine-6-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(3-phenylpyrrolidin-1-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-(1,3-dihydro-2H-isoindol-2-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[3-(tetrahydrofuran-2-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)butyl]-3-imidazo[1,2-a]pyridin-6-ylurea;-   2-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[2-oxo-4-(tetrahydrofuran-3-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(2-oxo-5-phenyl-1,3-oxazolidin-3-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methyl-1,3-thiazol-5-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methyl-1,3-thiazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(3-methyl-1,2-oxazol-5-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(3-chloro-1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(3-methoxy-1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(3,5-dimethyl-1,2-oxazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-{[3-(3,5-dimethyl-1,2-oxazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1-methyl-1H-pyrazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(4-methyl-1,3-thiazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-2-ylmethyl)(1H-tetrazol-5-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(1,2-oxazol-3-ylacetyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1,2-oxazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-2-ylmethyl)    [3-(1,3-thiazol-2-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydrofuran-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-3-ylmethyl)(tetrahydro-2H-pyran-4-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydrofuran-3-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-3-ylcarbonyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydro-2H-pyran-4-ylcarbonyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(3-methoxypropanoyl)[(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-3-ylcarbonyl)    [(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2R)-tetrahydrofuran-2-ylmethyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(3-methoxypropanoyl)    [(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-3-ylcarbonyl)    [(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2S)-tetrahydrofuran-2-ylmethyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydro-2H-pyran-4-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-({[2-(propan-2-yloxy)ethyl]carbamoyl}[(2R)-tetrahydrofuran-2-ylmethyl]amino)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl][(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-({[2-(propan-2-yloxy)ethyl]carbamoyl}[(2S)-tetrahydrofuran-2-ylmethyl]amino)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-[5-(4-chlorophenyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;-   4-[(1-butanoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(3-methoxy-2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropanoyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(cyclohexylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2R)-2-hydroxybutyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(1-methyl-1H-pyrazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethyl-1H-pyrazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4S)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   2-{(4R)-4-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-{(4S)-4-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1-methyl-1H-pyrrol-2-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,5-dimethyl-1H-pyrazol-3-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-2-ylmethyl)(1,3-thiazol-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(1,2-oxazol-3-ylacetyl)[(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(5-methyl-1,2-oxazol-3-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1,2-oxazol-5-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1,2-oxazol-4-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(2R)-tetrahydrofuran-2-ylmethyl](1,3-thiazol-4-ylacetyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,5-dimethyl-1H-pyrazol-3-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1-methyl-1H-pyrazol-4-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(3,5-dimethyl-1,2-oxazol-4-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(1-methyl-1H-pyrazol-4-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1-methyl-1H-pyrrol-2-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   2-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   tert-butyl    {4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[3-(tetrahydrofuran-2-yl)propanoyl]amino}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide;    4-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(4-methylpentanoyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   4-[(4-cyanobenzyl)(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   2-{5-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   4-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   5-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]thiophene-2-carboxamide;-   1-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   2-[(2S)-2-(hydroxymethyl)-5-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4R)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   5-[1-(cyclopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]thiophene-2-carboxamide;-   2-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(5S)-2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(5R)-2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methoxyacetyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   1-[4-(1-benzoylpiperidin-4-yl)butyl]-3-imidazo[1,2-a]pyridin-7-ylurea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(cyclohexylmethyl)-5-ethyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methoxy-3,3-dimethylcyclohexyl)methyl]-5-methyl-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide;-   3-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)propanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(propan-2-yloxy)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydrofuran-2-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-3-phenylpropanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide;-   3-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)propanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(propan-2-yloxy)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydrofuran-2-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3-phenylpropanamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   tert-butyl    4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylate;-   tert-butyl    (3R)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylate;-   tert-butyl    {2-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(morpholin-4-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-(1-ethyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(1,1-dioxidotetrahydrothiophen-3-yl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-phenylthiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(methylsulfonyl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}pyrrolidine-1-carboxylate;-   tert-butyl    3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)pyrrolidine-1-carboxylate;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)biphenyl-2-sulfonamide;-   5-{1-[(2R)-2-hydroxypropyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[(cyclopentylacetyl)amino]-3-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-{2-fluoro-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   4-[1-(cyclopropylacetyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   tert-butyl    4-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(propan-2-yloxy)phenyl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   tert-butyl    4-[4-(imidazo[1,2-a]pyridin-7-ylcarbamoyl)phenyl]piperidine-1-carboxylate;-   tert-butyl    4-[4-(imidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl]piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(2-methylpropanoyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   5-[3-(benzoylamino)oxetan-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(tetrahydrofuran-3-ylacetyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(pentanoylamino)oxetan-3-yl]thiophene-2-carboxamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(4-{[(3R)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(4-{[(3R)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3R)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}benzamide;-   5-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-3-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(3-methoxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-butanoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(3-hydroxy-3-methylbutanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2-(4-benzoylpiperazin-1-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(propan-2-yl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-phenyl-1,3-thiazole-5-carboxamide;-   1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide;-   tert-butyl    3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)azetidine-1-carboxylate;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]benzamide;-   1-[4-(1-acetylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}phenyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4-ylacetyl)pyrrolidin-3-yl]phenyl}urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   4-{[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]amino}-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-6-yl)methyl]-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   5-(4-hydroxytetrahydro-2H-pyran-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}azetidine-1-carboxylate;-   tert-butyl    4-hydroxy-4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[5-(piperidin-1-ylcarbonyl)-1,3-thiazol-2-yl]urea;-   5-{3-hydroxy-1-[(2S)-2-methylbutanoyl]azetidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(3-{[(2S)-2-methylbutanoyl]amino}oxetan-3-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1-[1-(3-methylbutanoyl)piperidin-4-yl]-1H-pyrazole-3-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   1-{4-[(1-acetylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[(1-benzoylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(propan-2-yloxy)acetyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(4-{[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)urea;-   1-(4-{[1-(1,4-dioxan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)urea;-   tert-butyl    (3R)-3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}pyrrolidine-1-carboxylate;-   4-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-{1-[(3,3-difluorocyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[(1-benzoylpiperidin-4-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)azetidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylazetidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(propan-2-yloxy)acetyl]azetidin-3-yl}phenyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]phenyl}urea;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[6-(morpholin-4-yl)pyridin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methyltetrahydro-2H-pyran-2-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylbutanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-{[(2S)-2-methylbutanoyl]amino}cyclobutyl)thiophene-2-carboxamide;-   5-[1-(benzoylamino)cyclobutyl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3,3,3-trifluoropropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(1-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}cyclobutyl)tetrahydro-2H-pyran-4-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}azetidine-1-carboxylate;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   4-[1-(furan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(piperidin-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-phenoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)azetidin-3-yl]benzamide;-   tert-butyl    4-{4-[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-phenoxyphenyl)urea;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2,2-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohexylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   4-(1-butanoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylpent-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyloxetan-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopropyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopentylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-oxobutanoyl)piperidin-4-yl]benzamide;-   4-{1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-propanoylpiperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(2,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)azetidin-3-yl]benzamide;-   5-[4-hydroxy-1-(3-methylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[4-hydroxy-1-(2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-4-hydroxypiperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylazetidin-3-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   tert-butyl    4-{4-[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   2-cyclopentyl-N-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   tert-butyl    4-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-1-ylcarbonyl)benzamide;-   4-[1-(ethylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)azetidin-3-yl]benzamide;-   propan-2-yl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   2-methylpropyl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(2-cyano-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3R)-tetrahydrofuran-3-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}benzamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(ethylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)azetidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)azetidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)azetidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)pyrrolidin-3-yl]benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide;-   4-[1-(cyclopropylsulfonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-{(1R)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{(1R)-3-methyl-1-[(tetrahydrofuran-3-ylacetyl)amino]butyl}thiophene-2-carboxamide;-   5-{(1S)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1-phenylpiperidin-4-yl)-1,3-thiazole-5-carboxamide;-   1-(4-{[(3R)-1-(2-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(3-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(4-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(4-{[(3R)-1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(2-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(4-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(pyridin-2-yl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   1-[4-(1-butanoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopropyl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(phenylacetyl)piperidin-4-yl]phenyl}urea;-   5-[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4-methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   1-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3-fluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(2,4-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(2,5-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3,4-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3,5-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)pyrrolidin-3-yl]benzamide;    N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methyl-2-phenylpropanoyl)pyrrolidin-3-yl]benzamide;-   4-{1-[difluoro(phenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]furan-2-carboxamide;-   4-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   5-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[4-(2-methylpropyl)phenyl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-2-methylbutanoyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{1-[(2-methylpropyl)sulfonyl]pyrrolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(phenylsulfonyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidine-1-carboxylate;-   5-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-{1-[(3-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(3,5-difluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2E)-2-methylpent-2-enoyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-{1-[(2,5-dimethylfuran-3-yl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propanoylpyrrolidin-3-yl)thiophene-2-carboxamide;-   5-{1-[(1-cyanocyclopropyl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-butanoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyrazin-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(phenylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   2-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   5-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   2-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-[2-(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)ethyl]piperazine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutyl)-1H-pyrazol-5-yl]furan-2-carboxamide;-   5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(3-methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-methylbutanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(1-methylpiperidin-4-yl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}acetamide;-   tert-butyl    4-{4-[(imidazo[1,2-b]pyridazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-b]pyridazin-6-ylmethyl)benzamide;-   5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(propan-2-ylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(phenylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}piperidine-1-carboxylate;-   N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide;-   2-(imidazo[1,2-a]pyridin-6-yl)-N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}acetamide;-   N-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2-methoxyphenyl)acetyl]amino}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(phenylacetyl)amino]benzamide;-   4-(benzoylamino)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   3,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   3,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   2,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   2-fluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-3-methoxybenzamide;-   4-{[(2-fluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-methyl-2-(piperazin-1-yl)propanoyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-2-methoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(phenylsulfonyl)benzamide;-   4-(phenylsulfonyl)-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)benzamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-oxatricyclo[3.3.1.1˜3,7˜]dec-1-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   4-{[(2,5-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(2,4-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-cyclopropyl-1-(2-methoxyethyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   4-{[difluoro(phenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(2-methyl-2-phenylpropanoyl)amino]benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(phenylsulfonyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(phenylsulfonyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylate;-   N-[(3-chloroimidazo[1,2-a]pyrazin-6-yl)methyl]-4-[(cyclopentylacetyl)amino]benzamide;-   N-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   2-(imidazo[1,2-a]pyridin-7-yl)-N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}acetamide;-   1-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-methyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide;-   5-[1-benzyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   N-(2,5-difluorobenzyl)-N′-(imidazo[1,2-a]pyridin-7-ylmethyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(propan-2-yl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-{4-[5-(2,2-dimethylpropyl)-1,3,4-oxadiazol-2-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   tert-butyl    4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbut-2-enoyl)piperidin-4-yl]benzamide;-   4-[1-(3-fluoro-4-methoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopent-1-en-1-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-ethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxyphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2-acetylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(methoxymethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-phenylpropanoyl)piperidin-4-yl]benzamide;-   4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[(2-methylpropyl)sulfonyl]acetyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-phenoxypropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-({[(1R,2S)-2-methylcyclohexyl]oxy}acetyl)piperidin-4-yl]benzamide;-   4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methoxyphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylbut-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5-methylphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-(4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3-methylbut-2-enoyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopent-1-en-1-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2-ethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,4-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,5-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-oxo-2,3-dihydro-1H-inden-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-2-methylbut-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(1H-indol-3-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-4,5,6,7-tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(pyridin-2-yl)cyclopropyl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-dihydro-2H-chromen-6-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(cyclohexyloxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloropyridin-3-yl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-cyclopropyl-1,2-oxazol-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2H-chromen-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-1,3-benzoxazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thieno[3,2-b]pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinolin-7-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(5,6,7,8-tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-7-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinoxalin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(2-methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(pyridin-2-yl)prop-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(8-methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methyl-4H-furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-8-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[3-methyl-1-(prop-2-en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)benzamide;-   4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)tetrahydro-2H-pyran-4-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxy-6-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(4-{1-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-4,5,6,7-tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(4-{-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(pyridin-2-yl)cyclopropyl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,3-dihydro-1-benzofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-1,3-benzoxazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(cinnolin-4-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinolin-7-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(5,6,7,8-tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-7-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinoxalin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(2-methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(pyridin-2-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-2,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(8-methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methyl-4H-furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2,3-dihydro-1-benzofuran-5-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-1-ethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-8-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[3-methyl-1-(prop-2-en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-{4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-methyl-5-(propan-2-yl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide;-   1-(4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   tert-butyl    4-{3-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]benzamide;-   1-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(4-methylpentanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(2-fluoro-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2-cyanobenzoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-N,N-dimethylpiperidine-1-carboxamide;-   1-{2-fluoro-4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-[(cyclopentylacetyl)amino]-N-[(7-fluoroimidazo[1,2-a]pyridin-6-yl)methyl]benzamide;-   N-[(7-fluoroimidazo[1,2-a]pyridin-6-yl)methyl]-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   5-{1-[2,2-dimethyl-3-(piperazin-1-yl)propyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-amino-2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]acetyl}piperidin-4-yl)benzamide;-   4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-1-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxy-5-methylpyridin-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[4-(propan-2-yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-5-propyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2,3-dihydro-1-benzofuran-7-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3-thiazol-4-yl]carbonyl}piperidin-4-yl)benzamide;-   4-(1-{[1-(difluoromethyl)-5-methyl-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazolo[1,5-a]pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3-oxazol-4-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5-methylpyridin-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide;-   1-(4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(thieno[3,2-b]furan-5-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxy-5-methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[4-(propan-2-yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-5-propyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(pyrazolo[1,5-a]pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(propan-2-yl)-1,3-oxazol-4-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-7-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxy-5-methylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H-indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H-indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[6-(trifluoromethyl)pyrimidin-4-yl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   5-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   4-(1-benzoylpiperidin-4-yl)-2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-({4-methyl-1-[2-(piperazin-1-yl)ethyl]piperidin-4-yl}methyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   S-(2-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-2-oxoethyl)-L-cysteine;-   5-(1-{[1-(15-amino-4,7,10,13-tetraoxapentadecan-1-oyl)-4-methylpiperidin-4-yl]methyl}-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   S-{2-[(3-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-3-oxopropyl)amino]-2-oxoethyl}-L-cysteine;    and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds of Formula (IA), selectedfrom the group consisting of

-   4-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluoro-4-methoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2-acetylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(methoxymethyl)benzoyl]piperidin-4-yl}benzamide;-   4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxy-6-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;    and pharmaceutically acceptable salts thereof.

Another embodiment pertains to a composition for treating inflammatoryand tissue repair disorders; particularly rheumatoid arthritis,inflammatory bowel disease, asthma and COPD (chronic obstructivepulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases;dermatosis, including psoriasis, atopic dermatitis and ultra-violetinduced skin damage; autoimmune diseases including systemic upuserythematosis, multiple sclerosis, psoriatic arthritis, ankylosingspondylitis, tissue and organ rejection, Alzheimer's disease, stroke,athersclerosis, restenosis, diabetes, glomerulonephritis, cancer,particularly wherein the cancer is selected from breast, prostate, lung,colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphomaor Hodgkin's disease, cachexia, inflammation associated with infectionand certain viral infections, including Acquired Immune DeficiencySyndrome (AIDS), adult respiratory distress syndrome, and ataxiatelengiectasia, said composition comprising an excipient and atherapeutically effective amount of a compound of Formula (IB), orpharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating inflammatory andtissue repair disorders; particularly rheumatoid arthritis, inflammatorybowel disease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia in apatient, said method comprising administering to the patient atherapeutically effective amount of a compound of Formula (IB), orpharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating inflammatory andtissue repair disorders; particularly rheumatoid arthritis, inflammatorybowel disease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia or spleencancer in a patient, said method comprising administering to the patienttherapeutically effective amount of the compound of Formula (IB), orpharmaceutically acceptable salts thereof; and a therapeuticallyeffective amount of one additional therapeutic agent or more than oneadditional therapeutic agent.

DETAILED DESCRIPTION OF THE INVENTION

This detailed description is intended only to acquaint others skilled inthe art with Applicants' invention, its principles, and its practicalapplication so that others skilled in the art may adapt and apply theinvention in its numerous forms, as they may be best suited to therequirements of a particular use. This description and its specificexamples are intended for purposes of illustration only. This invention,therefore, is not limited to the embodiments described in this patentapplication, and may be variously modified.

ABBREVIATIONS AND DEFINITIONS

Unless otherwise defined herein, scientific and technical terms used inconnection with the present invention shall have the meanings that arecommonly understood by those of ordinary skill in the art. The meaningand scope of the terms should be clear, however, in the event of anylatent ambiguity, definitions provided herein take precedent over anydictionary or extrinsic definition. In this application, the use of “or”means “and/or” unless stated otherwise. Furthermore, the use of the term“including”, as well as other forms, such as “includes” and “included”,is not limiting. With reference to the use of the words “comprise” or“comprises” or “comprising” in this patent application (including theclaims), Applicants note that unless the context requires otherwise,those words are used on the basis and clear understanding that they areto be interpreted inclusively, rather than exclusively, and thatApplicants intend each of those words to be so interpreted in construingthis patent application, including the claims below. For a variable thatoccurs more than one time in any substituent or in the compound of theinvention or any other formulae herein, its definition on eachoccurrence is independent of its definition at every other occurrence.Combinations of substituents are permissible only if such combinationsresult in stable compounds. Stable compounds are compounds which can beisolated in a useful degree of purity from a reaction mixture.

It is meant to be understood that proper valences are maintained for allcombinations herein, that monovalent moieties having more than one atomare attached through their left ends, and that divalent moieties aredrawn from left to right.

As used in the specification and the appended claims, unless specifiedto the contrary, the following terms have the meaning indicated:

The term “alkyl” (alone or in combination with another term(s)) means astraight- or branched-chain saturated hydrocarbyl substituent typicallycontaining from 1 to about 10 carbon atoms; or in another embodiment,from 1 to about 8 carbon atoms; in another embodiment, from 1 to about 6carbon atoms; and in another embodiment, from 1 to about 4 carbon atoms.Examples of such substituents include methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, iso-amyl,and hexyl and the like.

The term “alkenyl” (alone or in combination with another term(s)) meansa straight- or branched-chain hydrocarbyl substituent containing one ormore double bonds and typically from 2 to about 10 carbon atoms; or inanother embodiment, from 2 to about 8 carbon atoms; in anotherembodiment, from 2 to about 6 carbon atoms; and in another embodiment,from 2 to about 4 carbon atoms. Examples of such substituents includeethenyl (vinyl), 2-propenyl, 3-propenyl, 1,4-pentadienyl,1,4-butadienyl, 1-butenyl, 2-butenyl, and 3-butenyl and the like.

The term “alkynyl” (alone or in combination with another term(s)) meansa straight- or branched-chain hydrocarbyl substituent containing one ormore triple bonds and typically from 2 to about 10 carbon atoms; or inanother embodiment, from 2 to about 8 carbon atoms; in anotherembodiment, from 2 to about 6 carbon atoms; and in another embodiment,from 2 to about 4 carbon atoms. Examples of such substituents includeethynyl, 2-propynyl, 3-propynyl, 2-butynyl, and 3-butynyl and the like.

The term “carbocyclyl” (alone or in combination with another term(s))means a saturated cyclic (i.e., “cycloalkyl”), partially saturatedcyclic (i.e., “cycloalkenyl”), or completely unsaturated (i.e., “aryl”)hydrocarbyl substituent containing from 3 to 14 carbon ring atoms (“ringatoms” are the atoms bound together to form the ring or rings of acyclic substituent). A carbocyclyl may be a single-ring (monocyclic) orpolycyclic ring structure.

A carbocyclyl may be a single ring structure, which typically containsfrom 3 to 8 ring atoms, more typically from 3 to 6 ring atoms, and evenmore typically 5 to 6 ring atoms. Examples of such single-ringcarbocyclyls include cyclopropyl (cyclopropanyl), cyclobutyl(cyclobutanyl), cyclopentyl (cyclopentanyl), cyclopentenyl,cyclopentadienyl, cyclohexyl (cyclohexanyl), cyclohexenyl,cyclohexadienyl, and phenyl. A carbocyclyl may alternatively bepolycyclic (i.e., may contain more than one ring). Examples ofpolycyclic carbocyclyls include bridged, fused, and spirocycliccarbocyclyls. In a spirocyclic carbocyclyl, one atom is common to twodifferent rings. An example of a spirocyclic carbocyclyl isspiropentanyl. In a bridged carbocyclyl, the rings share at least twocommon non-adjacent atoms. Examples of bridged carbocyclyls includebicyclo[2.2.1]heptanyl, bicyclo[2.2.1]hept-2-enyl, and adamantanyl. In afused-ring carbocyclyl system, two or more rings may be fused together,such that two rings share one common bond. Examples of two- orthree-fused ring carbocyclyls include naphthalenyl,tetrahydronaphthalenyl (tetralinyl), indenyl, indanyl (dihydroindenyl),anthracenyl, phenanthrenyl, and decalinyl.

The term “cycloalkyl” (alone or in combination with another term(s))means a saturated cyclic hydrocarbyl substituent containing from 3 to 14carbon ring atoms. A cycloalkyl may be a single carbon ring, whichtypically contains from 3 to 8 carbon ring atoms and more typically from3 to 6 ring atoms. Examples of single-ring cycloalkyls includecyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. A cycloalkyl mayalternatively be polycyclic or contain more than one ring. Examples ofpolycyclic cycloalkyls include bridged, fused, and spirocycliccarbocyclyls.

The term “aryl” (alone or in combination with another term(s)) means anaromatic carbocyclyl containing from 6 to 14 carbon ring atoms. An arylmay be monocyclic or polycyclic (i.e., may contain more than one ring).In the case of polycyclic aromatic rings, only one ring the polycyclicsystem is required to be unsaturated while the remaining ring(s) may besaturated, partially saturated or unsaturated. Examples of aryls includephenyl, naphthalenyl, indenyl, indanyl, and tetrahydronapthyl.

In some instances, the number of carbon atoms in a hydrocarbylsubstituent (e.g., alkyl, alkenyl, alkynyl, or cycloalkyl) is indicatedby the prefix “C_(x)-C_(y)-”, wherein x is the minimum and y is themaximum number of carbon atoms in the substituent. Thus, for example,“C₁-C₆-alkyl” refers to an alkyl substituent containing from 1 to 6carbon atoms. Illustrating further, C₃-C₈-cycloalkyl means a saturatedhydrocarbyl ring containing from 3 to 8 carbon ring atoms.

The term “hydrogen” (alone or in combination with another term(s)) meansa hydrogen radical, and may be depicted as —H.

The term “hydroxy” (alone or in combination with another term(s)) means—OH.

The term “carboxy” (alone or in combination with another term(s)) means—C(O)—OH.

The term “amino” (alone or in combination with another term(s)) means—NH₂.

The term “halogen” or “halo” (alone or in combination with anotherterm(s)) means a fluorine radical (which may be depicted as —F),chlorine radical (which may be depicted as —Cl), bromine radical (whichmay be depicted as —Br), or iodine radical (which may be depicted as—I).

If a substituent is described as being “substituted”, a non-hydrogenradical is in the place of hydrogen radical on a carbon or nitrogen ofthe substituent. Thus, for example, a substituted alkyl substituent isan alkyl substituent in which at least one non-hydrogen radical is inthe place of a hydrogen radical on the alkyl substituent. To illustrate,monofluoroalkyl is alkyl substituted with a fluoro radical, anddifluoroalkyl is alkyl substituted with two fluoro radicals. It shouldbe recognized that if there are more than one substitution on asubstituent, each non-hydrogen radical may be identical or different(unless otherwise stated).

If a substituent is described as being “optionally substituted”, thesubstituent may be either (1) not substituted or (2) substituted. If asubstituent is described as being optionally substituted with up to aparticular number of non-hydrogen radicals, that substituent may beeither (1) not substituted; or (2) substituted by up to that particularnumber of non-hydrogen radicals or by up to the maximum number ofsubstitutable positions on the substituent, whichever is less. Thus, forexample, if a substituent is described as a heteroaryl optionallysubstituted with up to 3 non-hydrogen radicals, then any heteroaryl withless than 3 substitutable positions would be optionally substituted byup to only as many non-hydrogen radicals as the heteroaryl hassubstitutable positions. To illustrate, tetrazolyl (which has only onesubstitutable position) would be optionally substituted with up to onenon-hydrogen radical. To illustrate further, if an amino nitrogen isdescribed as being optionally substituted with up to 2 non-hydrogenradicals, then a primary amino nitrogen will be optionally substitutedwith up to 2 non-hydrogen radicals, whereas a secondary amino nitrogenwill be optionally substituted with up to only 1 non-hydrogen radical.

This patent application uses the terms “substituent” and “radical”interchangeably.

The prefix “halo” indicates that the substituent to which the prefix isattached is substituted with one or more independently selected halogenradicals. For example, haloalkyl means an alkyl substituent in which atleast one hydrogen radical is replaced with a halogen radical. Examplesof haloalkyls include chloromethyl, 1-bromoethyl, fluoromethyl,difluoromethyl, trifluoromethyl, and 1,1,1-trifluoroethyl. It should berecognized that if a substituent is substituted by more than one halogenradical, those halogen radicals may be identical or different (unlessotherwise stated).

The prefix “perhalo” indicates that every hydrogen radical on thesubstituent to which the prefix is attached is replaced withindependently selected halogen radicals, i.e., each hydrogen radical onthe substituent is replaced with a halogen radical. If all the halogenradicals are identical, the prefix typically will identify the halogenradical. Thus, for example, the term “perfluoro” means that everyhydrogen radical on the substituent to which the prefix is attached issubstituted with a fluorine radical. To illustrate, the term“perfluoroalkyl” means an alkyl substituent wherein a fluorine radicalis in the place of each hydrogen radical.

The term “carbonyl” (alone or in combination with another term(s)) means—C(O)—.

The term “aminocarbonyl” (alone or in combination with another term(s))means —C(O)—NH₂.

The term “oxo” (alone or in combination with another term(s)) means(═O).

The term “oxy” (alone or in combination with another term(s)) means anether substituent, and may be depicted as —O—.

The term “alkylhydroxy” (alone or in combination with another term(s))means -alkyl-OH.

The term “alkylamino” (alone or in combination with another term(s))means -alkyl-NH₂.

The term “alkyloxy” (alone or in combination with another term(s)) meansan alkylether substituent, i.e., —O-alkyl. Examples of such asubstituent include methoxy (—O—CH₃), ethoxy, n-propoxy, isopropoxy,n-butoxy, iso-butoxy, sec-butoxy, and tert-butoxy.

The term “alkylcarbonyl” (alone or in combination with another term(s))means —C(O)-alkyl.

The term “aminoalkylcarbonyl” (alone or in combination with anotherterm(s)) means —C(O)-alkyl-NH₂.

The term “alkyloxycarbonyl” (alone or in combination with anotherterm(s)) means —C(O)—O-alkyl.

The term “carbocyclylcarbonyl” (alone or in combination with anotherterm(s)) means —C(O)-carbocyclyl.

Similarly, the term “heterocyclylcarbonyl” (alone or in combination withanother term(s)) means —C(O)-heterocyclyl.

The term “carbocyclylalkylcarbonyl” (alone or in combination withanother term(s)) means —C(O)-alkyl-carbocyclyl.

Similarly, the term “heterocyclylalkylcarbonyl” (alone or in combinationwith another term(s)) means —C(O)-alkyl-heterocyclyl.

The term “carbocyclyloxycarbonyl” (alone or in combination with anotherterm(s)) means —C(O)—O-carbocyclyl.

The term “carbocyclylalkyloxycarbonyl” (alone or in combination withanother term(s)) means —C(O)—O-alkyl-carbocyclyl.

The term “thio” or “thia” (alone or in combination with another term(s))means a thiaether substituent, i.e., an ether substituent wherein adivalent sulfur atom is in the place of the ether oxygen atom. Such asubstituent may be depicted as —S—. This, for example,“alkyl-thio-alkyl” means alkyl-S-alkyl (alkyl-sulfanyl-alkyl).

The term “thiol” or “sulfhydryl” (alone or in combination with anotherterm(s)) means a sulfhydryl substituent, and may be depicted as —SH.

The term “(thiocarbonyl)” (alone or in combination with another term(s))means a carbonyl wherein the oxygen atom has been replaced with asulfur. Such a substituent may be depicted as —C(S)—.

The term “sulfonyl” (alone or in combination with another term(s)) means—S(O)₂—.

The term “aminosulfonyl” (alone or in combination with another term(s))means —S(O)₂—NH₂.

The term “sulfinyl” or “sulfoxido” (alone or in combination with anotherterm(s)) means —S(O)—.

The term “heterocyclyl” (alone or in combination with another term(s))means a saturated (i.e., “heterocycloalkyl”), partially saturated (i.e.,“heterocycloalkenyl”), or completely unsaturated (i.e., “heteroaryl”)ring structure containing a total of 3 to 14 ring atoms. At least one ofthe ring atoms is a heteroatom (i.e., oxygen, nitrogen, or sulfur), withthe remaining ring atoms being independently selected from the groupconsisting of carbon, oxygen, nitrogen, and sulfur. A heterocyclyl maybe a single-ring (monocyclic) or polycyclic ring structure.

A heterocyclyl may be a single ring, which typically contains from 3 to7 ring atoms, more typically from 3 to 6 ring atoms, and even moretypically 5 to 6 ring atoms. Examples of single-ring heterocyclylsinclude 1,2,3,6-tetrahydropyridine, thiomorpholinyl, tetrahydropyranyl,furanyl, dihydrofuranyl, tetrahydrofuranyl, thiophenyl (thiofuranyl),dihydrothiophenyl, tetrahydrothiophenyl, pyrrolyl, pyrrolinyl,pyrrolidinyl, imidazolyl, imidazolinyl, imidazolidinyl, pyrazolyl,pyrazolinyl, pyrazolidinyl, triazolyl, tetrazolyl, oxazolyl,oxazolidinyl, isoxazolidinyl, isoxazolyl, thiazolyl, isothiazolyl,thiazolinyl, isothiazolinyl, thiazolidinyl, isothiazolidinyl,thiodiazolyl, oxadiazolyl (including 1,2,3-oxadiazolyl,1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl (furazanyl), or 1,3,4-oxadiazolyl),oxatriazolyl (including 1,2,3,4-oxatriazolyl or 1,2,3,5-oxatriazolyl),dioxazolyl (including 1,2,3-dioxazolyl, 1,2,4-dioxazolyl,1,3,2-dioxazolyl, or 1,3,4-dioxazolyl), oxathiazolyl, oxathiolyl,oxathiolanyl, pyranyl, dihydropyranyl, thiopyranyl,tetrahydrothiopyranyl, pyridinyl (azinyl), piperidinyl, diazinyl(including pyridazinyl (1,2-diazinyl), pyrimidinyl (1,3-diazinyl), orpyrazinyl (1,4-diazinyl)), piperazinyl, pyrrolidin-2-only, triazinyl(including 1,3,5-triazinyl, 1,2,4-triazinyl, and 1,2,3-triazinyl)),oxazinyl (including 1,2-oxazinyl, 1,3-oxazinyl, or 1,4-oxazinyl)),oxathiazinyl (including 1,2,3-oxathiazinyl, 1,2,4-oxathiazinyl,1,2,5-oxathiazinyl, or 1,2,6-oxathiazinyl)), oxadiazinyl (including1,2,3-oxadiazinyl, 1,2,4-oxadiazinyl, 1,4,2-oxadiazinyl, or1,3,5-oxadiazinyl)), morpholinyl, azepinyl, oxepinyl, thiepinyl, anddiazepinyl.

A heterocyclyl may alternatively be polycyclic (i.e., may contain morethan one ring). Examples of polycyclic heterocyclyls include bridged,fused, and spirocyclic heterocyclyls. In a spirocyclic heterocyclyl, oneatom is common to two different rings. In a bridged heterocyclyl, therings share at least two common non-adjacent atoms. In a fused-ringheterocyclyl, two or more rings may be fused together, such that tworings share one common bond. Examples of fused-ring heterocyclylsinclude hexahydro-furo[3,4-c]pyrrole, hexahydro-furo[3,4-b]pyrrole,octahydro-pyrrolo[3,4-b]pyridine, octahydro-pyrrolo[3,4-c]pyridine,(3aR,6aR)-5-methyl-octahydro-pyrrolo[3,4-b]pyrrole,(3aR,6aR)-octahydro-pyrrolo[3,4-b]pyrrole,6-methyl-2,6-diaza-bicyclo[3.2.0]heptane,(3aS,6aR)-2-methyl-octahydro-pyrrolo[3,4-c]pyrrole,decahydro-[1,5]naphthyridine, 2,3-dihydrobenzofuranyl,2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indolyl, thieno[3,2-c]pyridinyl,furo[3,2-c]pyridinyl, phthalazin-1(2H)-onyl, isoquinolinyl,isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl,fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl,(trifluoromethyl)phthalazin-1(2H)-onyl,pyrrolo[1,2-d][1,2,4]triazin-1(2H)-onyl,1,2,3,4-tetrahydroisoquinolinyl, 2,3-dihydrobenzo[b][1,4]dioxinyl,5,6,7,8-tetrahydrophthalazin-1(2H)-onyl,5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl,5,6,7,8-tetrahydroimidazo[1,5-a]pyrazinyl, thieno[3,2-c]pyridinyl,furo[3,2-c]pyridinyl, indolizinyl, pyranopyrrolyl, 4H-quinolizinyl,purinyl, naphthyridinyl, pyridopyridinyl (includingpyrido[3,4-b]-pyridinyl, pyrido[3,2-b]-pyridinyl, orpyrido[4,3-b]-pyridinyl), and pteridinyl. Other examples of fused-ringheterocyclyls include benzo-fused heterocyclyls, such as benzimidazolyl,benzo[d][1,3]dioxolyl, indolyl, isoindolyl (isobenzazolyl,pseudoisoindolyl), indoleninyl (pseudoindolyl), isoindazolyl(benzpyrazolyl), benzazinyl (including quinolinyl (1-benzazinyl) orisoquinolinyl (2-benzazinyl)), phthalazinyl, quinoxalinyl, quinazolinyl,benzodiazinyl (including cinnolinyl (1,2-benzodiazinyl) or quinazolinyl(1,3-benzodiazinyl)), benzopyranyl (including chromanyl orisochromanyl), benzoxazinyl (including 1,3,2-benzoxazinyl,1,4,2-benzoxazinyl, 2,3,1-benzoxazinyl, or 3,1,4-benzoxazinyl), andbenzisoxazinyl (including 1,2-benzisoxazinyl or 1,4-benzisoxazinyl).Examples of spirocyclic heterocyclyls include1,4-dioxa-8-azaspiro[4.5]decanyl.

The term “5-6 membered heteroaryl” (alone or in combination with anotherterm(s)) means aromatic heterocyclyl containing a total of 5 to 6 ringatoms. At least one of the ring atoms is a heteroatom (i.e., oxygen,nitrogen, or sulfur), with the remaining ring atoms being independentlyselected from the group consisting of carbon, oxygen, nitrogen, andsulfur.

The term “heterocycloalkyl” (alone or in combination with anotherterm(s)) means a saturated heterocyclyl.

The term “heteroaryl” (alone or in combination with another term(s))means an aromatic heterocyclyl containing from 5 to 14 ring atoms. Aheteroaryl may be a single ring or 2 or 3 fused rings. Examples ofheteroaryl substituents include 6-membered ring substituents such aspyridyl, pyrazyl, pyrimidinyl, pyridazinyl, and 1,3,5-, 1,2,4- or1,2,3-triazinyl; 5-membered ring substituents such as imidazyl, furanyl,thiophenyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, 1,2,3-, 1,2,4-,1,2,5-, or 1,3,4-oxadiazolyl and isothiazolyl; 6/5-membered fused ringsubstituents such as benzothiofuranyl, benzisoxazolyl, benzoxazolyl, andpurinyl; and 6/6-membered fused rings such as benzopyranyl, quinolinyl,isoquinolinyl, cinnolinyl, quinazolinyl, and benzoxazinyl.

A prefix attached to a multi-component substituent only applies to thefirst component. To illustrate, the term “alkylcycloalkyl” contains twocomponents: alkyl and cycloalkyl. Thus, the C₁-C₆-prefix onC₁-C₆-alkylcycloalkyl means that the alkyl component of thealkylcycloalkyl contains from 1 to 6 carbon atoms; the C₁-C₆-prefix doesnot describe the cycloalkyl component. To illustrate further, the prefix“halo” on haloalkyloxyalkyl indicates that only the alkyloxy componentof the alkyloxyalkyl substituent is substituted with one or more halogenradicals. If halogen substitution may alternatively or additionallyoccur on the alkyl component, the substituent would instead be describedas “halogen-substituted alkyloxyalkyl” rather than “haloalkyloxyalkyl.”And finally, if the halogen substitution may only occur on the alkylcomponent, the substituent would instead be described as“alkyloxyhaloalkyl.”

The terms “treat”, “treating” and “treatment” refer to a method ofalleviating or abrogating a disease and/or its attendant symptoms.

The terms “prevent”, “preventing” and “prevention” refer to a method ofpreventing the onset of a disease and/or its attendant symptoms orbarring a subject from acquiring a disease. As used herein, “prevent”,“preventing” and “prevention” also include delaying the onset of adisease and/or its attendant symptoms and reducing a subject's risk ofacquiring a disease.

The term “therapeutically effective amount” refers to that amount of thecompound being administered sufficient to prevent development of oralleviate to some extent one or more of the symptoms of the condition ordisorder being treated.

The term “modulate” refers to the ability of a compound to increase ordecrease the function, or activity, of a kinase. “Modulation”, as usedherein in its various forms, is intended to encompass antagonism,agonism, partial antagonism and/or partial agonism of the activityassociated with kinase. Kinase inhibitors are compounds that, e.g., bindto, partially or totally block stimulation, decrease, prevent, delayactivation, inactivate, desensitize, or down regulate signaltransduction. Kinase activators are compounds that, e.g., bind to,stimulate, increase, open, activate, facilitate, enhance activation,sensitize or up regulate signal transduction.

The term “composition” as used herein is intended to encompass a productcomprising the specified ingredients in the specified amounts, as wellas any product which results, directly or indirectly, from combinationof the specified ingredients in the specified amounts. By“pharmaceutically acceptable” it is meant the carrier, diluent orexcipient must be compatible with the other ingredients of theformulation and not deleterious to the recipient thereof.

The “subject” is defined herein to include animals such as mammals,including, but not limited to, primates (e.g., humans), cows, sheep,goats, horses, dogs, cats, rabbits, rats, mice and the like. Inpreferred embodiments, the subject is a human.

Isotope Enriched or Labeled Compounds

Compounds of the invention can exist in isotope-labeled or -enrichedform containing one or more atoms having an atomic mass or mass numberdifferent from the atomic mass or mass number most abundantly found innature. Isotopes can be radioactive or non-radioactive isotopes.Isotopes of atoms such as hydrogen, carbon, phosphorous, sulfur,fluorine, chlorine, and iodine include, but are not limited to, ²H, ³H,¹³C, ¹⁴C, ¹⁵N, ¹⁸O, ³²P, ³⁵S, ¹⁸F, ³⁶Cl, and ¹²⁵I. Compounds thatcontain other isotopes of these and/or other atoms are within the scopeof this invention.

In another embodiment, the isotope-labeled compounds contain deuterium(²H), tritium (³H) or ¹⁴C isotopes. Isotope-labeled compounds of thisinvention can be prepared by the general methods well known to personshaving ordinary skill in the art. Such isotope-labeled compounds can beconveniently prepared by carrying out the procedures disclosed in theExamples disclosed herein and Schemes by substituting a readilyavailable isotope-labeled reagent for a non-labeled reagent. In someinstances, compounds may be treated with isotope-labeled reagents toexchange a normal atom with its isotope, for example, hydrogen fordeuterium can be exchanged by the action of a deuteric acid such asD₂SO₄/D₂O. In addition to the above, relevant procedures andintermediates are disclosed, for instance, in Lizondo, J et al., DrugsFut, 21(11), 1116 (1996); Brickner, S J et al., J Med Chem, 39(3), 673(1996); Mallesham, B et al., Org Lett, 5(7), 963 (2003); PCTpublications WO1997010223, WO2005099353, WO1995007271, WO2006008754;U.S. Pat. Nos. 7,538,189; 7,534,814; 7,531,685; 7,528,131; 7,521,421;7,514,068; 7,511,013; and US Patent Application Publication Nos.20090137457; 20090131485; 20090131363; 20090118238; 20090111840;20090105338; 20090105307; 20090105147; 20090093422; 20090088416; and20090082471, the methods are hereby incorporated by reference.

The isotope-labeled compounds of the invention may be used as standardsto determine the effectiveness in binding assays. Isotope containingcompounds have been used in pharmaceutical research to investigate thein vivo metabolic fate of the compounds by evaluation of the mechanismof action and metabolic pathway of the nonisotope-labeled parentcompound (Blake et al. J. Pharm. Sci. 64, 3, 367-391 (1975)). Suchmetabolic studies are important in the design of safe, effectivetherapeutic drugs, either because the in vivo active compoundadministered to the patient or because the metabolites produced from theparent compound prove to be toxic or carcinogenic (Foster et al.,Advances in Drug Research Vol. 14, pp. 2-36, Academic press, London,1985; Kato et al., J. Labelled Comp. Radiopharmaceut., 36(10):927-932(1995); Kushner et al., Can. J. Physiol. Pharmacol., 77, 79-88 (1999).

In addition, non-radio active isotope containing drugs, such asdeuterated drugs called “heavy drugs,” can be used for the treatment ofdiseases and conditions related to NAMPT activity. Increasing the amountof an isotope present in a compound above its natural abundance iscalled enrichment. Examples of the amount of enrichment include fromabout 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37,42, 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96, to about 100 mol%. Replacement of up to about 15% of normal atom with a heavy isotopehas been effected and maintained for a period of days to weeks inmammals, including rodents and dogs, with minimal observed adverseeffects (Czajka D M and Finkel A J, Ann. N.Y. Acad. Sci. 196084: 770;Thomson J F, Ann. New York Acad. Sci 1960 84: 736; Czakja D M et al.,Am. J. Physiol. 1961 201: 357). Acute replacement of as high as 15%-23%in human fluids with deuterium was found not to cause toxicity(Blagojevic N et al. in “Dosimetry & Treatment Planning for NeutronCapture Therapy”, Zamenhof R, Solares G and Harling O Eds. 1994.Advanced Medical Publishing, Madison Wis. pp. 125-134; Diabetes Metab.23: 251 (1997)).

Stable isotope labeling of a drug can alter its physico-chemicalproperties such as pKa and lipid solubility. These effects andalterations can affect the pharmacodynamic response of the drug moleculeif the isotopic substitution affects a region involved in aligand-receptor interaction. While some of the physical properties of astable isotope-labeled molecule are different from those of theunlabeled one, the chemical and biological properties are the same, withone important exception: because of the increased mass of the heavyisotope, any bond involving the heavy isotope and another atom will bestronger than the same bond between the light isotope and that atom.Accordingly, the incorporation of an isotope at a site of metabolism orenzymatic transformation will slow said reactions potentially alteringthe pharmacokinetic profile or efficacy relative to the non-isotopiccompound.

Compounds

Suitable groups for X, R¹, and Z in all Formulas are independentlyselected. The described embodiments of the present invention may becombined. Such combination is contemplated and within the scope of thepresent invention. For example, it is contemplated that embodiments forany of X, R¹, and Z can be combined with embodiments defined for anyother of X, R¹, and Z.

Embodiments of Formula (I)

One embodiment, therefore, pertains to compounds or pharmaceuticallyacceptable salts thereof, which are useful as inhibitors of NAMPT, thecompounds having Formula (I)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³; and CH₂NHC(O)R³; and

Z is CH or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is hydrogen;

Z is CR²; and

R² is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³; and CH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R^(3x) is independently selected from the group consisting of phenyl andheterocyclyl; wherein each R^(3x) phenyl and heterocyclyl is substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴,OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂,NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH,C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl;

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

m is 4, 5, or 6; and

n is 1 or 2;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is hydrogen; and R³is phenyl; the R³ phenyl is not substituted at the para position withphenyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

In one embodiment of Formula (I), X is N or CY¹. In another embodimentof Formula (I), X is N. In another embodiment of Formula (I), X is CY¹.

In one embodiment of Formula (I), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (I), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (I), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(I), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (I), Z is CH or N; R¹ is independentlyselected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and R² is hydrogen. In another embodimentof Formula (I), Z is CH or N; R¹ is NHC(O)NHR³; and R² is hydrogen. Inanother embodiment of Formula (I), Z is CH or N; R¹ isNHC(O)NH(CH₂)_(m)R^(3x); and R² is hydrogen. In another embodiment ofFormula (I), Z is CH or N; R¹ is CH₂NHC(O)NHR³; and R² is hydrogen. Inanother embodiment of Formula (I), Z is CH or N; R¹ is NHC(O)R³; and R²is hydrogen. In another embodiment of Formula (I), Z is CH or N; R¹ isNHC(O)(CH₂)_(n)R³; and R² is hydrogen. In another embodiment of Formula(I), Z is CH or N; R¹ is C(O)NH(CH₂)_(n)R³; and R² is hydrogen. Inanother embodiment of Formula (I), Z is CH or N; R¹ isNHC(O)(CH₂)_(m)R^(3x); and R² is hydrogen. In another embodiment ofFormula (I), Z is CH or N; R¹ is C(O)NH(CH₂)_(m)R^(3x); and R² ishydrogen. In another embodiment of Formula (I), Z is CH or N; R¹ isCH₂C(O)NHR³; and R² is hydrogen. In another embodiment of Formula (I), Zis CH or N; R¹ is CH₂NHC(O)R³; and R² is hydrogen.

In one embodiment of Formula (I), Z is CH; R¹ is independently selectedfrom the group consisting of NHC(O)NHR³, NHC(O)NH(CH₂)_(m)R^(3x),CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³, C(O)NH(CH₂)_(n)R³,NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x), CH₂C(O)NHR³, andCH₂NHC(O)R³; and R² is hydrogen. In another embodiment of Formula (I), Zis CH; R¹ is NHC(O)NHR³; and R² is hydrogen. In another embodiment ofFormula (I), Z is CH; R¹ is NHC(O)NH(CH₂)_(m)R^(3x); and R² is hydrogen.In another embodiment of Formula (I), Z is CH; R¹ is CH₂NHC(O)NHR³; andR² is hydrogen. In another embodiment of Formula (I), Z is CH; R¹ isNHC(O)R³; and R² is hydrogen. In another embodiment of Formula (I), Z isCH; R¹ is NHC(O)(CH₂)_(n)R³; and R² is hydrogen. In another embodimentof Formula (I), Z is CH; R¹ is C(O)NH(CH₂)_(n)R³; and R² is hydrogen. Inanother embodiment of Formula (I), Z is CH; R¹ is NHC(O)(CH₂)_(m)R^(3x);and R² is hydrogen. In another embodiment of Formula (I), Z is CH; R¹ isC(O)NH(CH₂)_(m)R^(3x); and R² is hydrogen. In another embodiment ofFormula (I), Z is CH; R¹ is CH₂C(O)NHR³; and R² is hydrogen. In anotherembodiment of Formula (I), Z is CH; R¹ is CH₂NHC(O)R³; and R² ishydrogen.

In one embodiment of Formula (I), Z is N; R¹ is independently selectedfrom the group consisting of NHC(O)NHR³, NHC(O)NH(CH₂)_(m)R^(3x),CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³, C(O)NH(CH₂)_(n)R³,NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x), CH₂C(O)NHR³, andCH₂NHC(O)R³; and R² is hydrogen. In another embodiment of Formula (I), Zis N; R¹ is NHC(O)NHR³; and R² is hydrogen. In another embodiment ofFormula (I), Z is N; R¹ is NHC(O)NH(CH₂)_(m)R^(3x); and R² is hydrogen.In another embodiment of Formula (I), Z is N; R¹ is CH₂NHC(O)NHR³; andR² is hydrogen. In another embodiment of Formula (I), Z is N; R¹ isNHC(O)R³; and R² is hydrogen. In another embodiment of Formula (I), Z isN; R¹ is NHC(O)(CH₂)_(n)R³; and R² is hydrogen. In another embodiment ofFormula (I), Z is N; R¹ is C(O)NH(CH₂)_(n)R³; and R² is hydrogen. Inanother embodiment of Formula (I), Z is N; R¹ is NHC(O)(CH₂)_(m)R^(3x);and R² is hydrogen. In another embodiment of Formula (I), Z is N; R¹ isC(O)NH(CH₂)_(m)R^(3x); and R² is hydrogen. In another embodiment ofFormula (I), Z is N; R¹ is CH₂C(O)NHR³; and R² is hydrogen. In anotherembodiment of Formula (I), Z is N; R¹ is CH₂NHC(O)R³; and R² ishydrogen.

In one embodiment of Formula (I), R¹ is hydrogen; Z is CR²; and R² isindependently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R³, C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (I), R¹is hydrogen; Z is CR²; and R² is NHC(O)NHR³. In another embodiment ofFormula (I), R¹ is hydrogen; Z is CR²; and R² isNHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula (I), R¹ ishydrogen; Z is CR²; and R² is CH₂NHC(O)NHR³. In another embodiment ofFormula (I), R¹ is hydrogen; Z is CR²; and R² is NHC(O)R³. In anotherembodiment of Formula (I), R¹ is hydrogen; Z is CR²; and R² isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (I), R¹ is hydrogen;Z is CR²; and R² is C(O)NH(CH₂)_(n)R³. In another embodiment of Formula(I), R¹ is hydrogen; Z is CR²; and R² is NHC(O)(CH₂)_(m)R^(3x). Inanother embodiment of Formula (I), R¹ is hydrogen; Z is CR²; and R² isC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula (I), R¹ ishydrogen; Z is CR²; and R² is CH₂C(O)NHR³. In another embodiment ofFormula (I), R¹ is hydrogen; Z is CR²; and R² is CH₂NHC(O)R³.

In one embodiment of Formula (I), m is 4, 5, or 6. In another embodimentof Formula (I), m is 4. In another embodiment of Formula (I), m is 5. Inanother embodiment of Formula (I), m is 6.

In one embodiment of Formula (I), n is 1 or 2. In another embodiment ofFormula (I), n is 1. In another embodiment of Formula (I), n is 2.

In one embodiment of Formula (I), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (I), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (I), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (I), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(I), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (I), R^(3x) is independently selected fromthe group consisting of phenyl and heterocyclyl; wherein each R^(3x)phenyl and heterocycyl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴,N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴,NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (I), R^(3x) is heterocyclyl;wherein each R^(3x) heterocycyl is substituted with C(O)R⁴, or CO(O)R⁴.

In one embodiment of Formula (I), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (I), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (I), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)², C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (I), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (I), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (I), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (I), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (I), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (I), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (I), R⁸ at each occurrence, isindependently alkyl.

In one embodiment of Formula (I), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (I), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (I), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (I), R¹⁰ at eachoccurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (I), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (I), R¹¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (I)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³; and CH₂NHC(O)R³; and

Z is CH or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen F,Cl, Br, and I;

R¹ is hydrogen;

Z is CR²; and

R² is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, CH₂C(O)NHR³; andCH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R^(3x) is independently heterocyclyl; wherein each R^(3x) heterocyclylis substituted with one substituents independently selected from thegroup consisting of C(O)R⁴, CO(O)R⁴, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl;

R¹¹ at each occurrence, is alkyl;

m is 4, or 5; and

n is 1;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is hydrogen; and R³is phenyl; the R³ phenyl is not substituted at the para position withphenyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

Still another embodiment pertains to compounds having Formula (I), whichincludes Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16,17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52,53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70,71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88,89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104,105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118,119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132,133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146,147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160,161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174,175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188,189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202,203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216,217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230,231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244,245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258,259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272,273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286,287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300,301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314,315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328,329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342,343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356,357, 358, 359, 360, 361, 362, 363, 364, 365, 366, 367, 368, 369, 370,371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384,385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398,399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412,413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426,427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440,441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454,455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468,469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482,483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496,497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510,511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524,525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538,539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552,553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566,567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580,580, 581, 582, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594,595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608,609, 610, 611, 612, 613, 614, 615, 616, 617, 618, 619, 620, 621, 622,623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636,637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650,651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664,665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677, 678,679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691, 692,693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706,707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719, 720,721, 722, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734,735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748,749, 750, 751, 752, 753, 754, 755, 756, 757, 758, 759, 760, 761, 762,763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773, 774, 775, 776,777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790,791, 792, 793, 794, 795, 796, 797, 798, 799, 800, 801, 802, 803, 804,805, 806, 807, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818,819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832,833, 834, 835, 836, 837, 838, 839, 840, 841, 842, 843, 844, 845, 846,847, 848, 849, 850, 851, 852, 853, 854, 855, 856, and pharmaceuticallyacceptable salts thereof.

Embodiments of Formula (II)

In another aspect, the present invention provides compounds of Formula(II)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (II) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (II), X is N or CY¹. In another embodimentof Formula (II), X is N. In another embodiment of Formula (II), X isCY¹.

In one embodiment of Formula (II), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (II), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (II), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(II), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (II), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (II), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (II), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (II), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(II), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (II), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (II), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (II), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (II), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (II), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (II), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (II), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (II), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (II), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (II), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (II), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (II), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (II), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (II), R¹⁰ at eachoccurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (II), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (II), R¹¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (II)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (II),which includes Example 2; and pharmaceutically acceptable salts thereof.

Embodiments of Formula (III)

In another aspect, the present invention provides compounds of Formula(III)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed in Formula (I) herein.

One embodiment pertains to compounds of Formula (III) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)², CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (III), X is N or CY¹. In another embodimentof Formula (III), X is N. In another embodiment of Formula (III), X isCY¹.

In one embodiment of Formula (III), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (III), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (III), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(III), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (III), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (III), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (III), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (III), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(III), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (III), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (III), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (III), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (III), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (III), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (III), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (III), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (III), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (III), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (III), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (III), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (III), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (III), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (III), R¹⁰ ateach occurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (III), R¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (III), R¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (III)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (III),which includes Examples 1, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15,16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33,34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51,89, 106, 109, 110, 111, 112, 113, 396, and pharmaceutically acceptablesalts thereof.

Embodiments of Formula (IV)

In another aspect, the present invention provides compounds of Formula(IV)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (IV) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IV), X is N or CY¹. In another embodimentof Formula (IV), X is N. In another embodiment of Formula (IV), X isCY¹.

In one embodiment of Formula (IV), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IV), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IV), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IV), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IV), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IV), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IV), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IV), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IV), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IV), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (IV), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IV), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IV), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IV), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IV), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IV), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (IV), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IV), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IV), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (IV), R¹⁰ at eachoccurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (IV), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IV), R¹¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IV)

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I; R⁴, at each occurrence, is independently selected from thegroup consisting of alkyl, aryl, cycloalkyl, and 3-12 memberedheterocyclyl; wherein each R⁴ alkyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; whereineach R⁴ aryl, cycloalkyl and 3-12 membered heterocyclyl is optionallysubstituted with one, or two substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IV),which includes Examples 118, 216, 220, 221, 222, 223, 224, 225, 226,227, 228, 229, 243, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289,290, 291, 302, 303, 306, 307, 328, 329, 330, 331, 332, 333, 334, 335,336, 337, 338, 364, 366, 379, 380, 381, 382, 383, 384, 385, 386, 387,388, 389, 390, 391, 392, 404, 407, 424, 425, 426, 427, 428, 429, 430,431, 432, 433, 434, 435, 438, 439, 442, 443, 444, 445, 446, 447, 448,449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 486,487, 496, 564, 565, 673, 674, 675, 689, 690, 691, 692, 693, 694, 695,696, 709, 710, 711, 712, 713, 714, 715, 716, 719, 720, 721, 722, 723,724, 725, 726, 727, 728, 729, 730, and pharmaceutically acceptable saltsthereof.

Embodiments of Formula (V)

In another aspect, the present invention provides compounds of Formula(V)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (V) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R₉, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl;

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (V), X is N or CY¹. In another embodimentof Formula (V), X is N. In another embodiment of Formula (V), X is CY¹.

In one embodiment of Formula (V), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (V), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (V), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(V), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (V), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (V), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (V), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (V), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(V), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (V), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (V), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (V), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (V), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (V), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (V), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (V), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (V), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (V), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (V), R⁸ at each occurrence, isindependently alkyl.

In one embodiment of Formula (V), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (V), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (V), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (V), R¹⁰ at eachoccurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (V), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (V), R¹¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (V)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (V), whichinclude Examples 59, 60, 274, 275, 276, 277, 278, 279, 360, 362, andpharmaceutically acceptable salts thereof.

Embodiments of Formula (VI)

In another aspect, the present invention provides compounds of Formula(VI)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (VI) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VI), X is N or CY¹. In another embodimentof Formula (VI), X is N. In another embodiment of Formula (VI), X isCY¹.

In one embodiment of Formula (VI), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VI), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VI), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VI), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VI), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VI), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VI), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (VI), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VI), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VI), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VI), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (VI), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VI), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VI), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VI), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VI), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VI), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (VI), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VI), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (VI), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VI), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VI), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (VI), R¹⁰ at eachoccurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (VI), R¹⁰ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VI), R¹⁰ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VI)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VI),which includes Examples 57, 117, 121, 138, 174, 181, 182, 185, 187, 188,192, 193, 194, 195, 196, 197, 198, 199, 202, 203, 204, 205, 207, 208,209, 210, 211, 212, 213, 214, 217, 218, 230, 231, 232, 233, 234, 235,236, 237, 238, 239, 241, 242, 244, 245, 246, 247, 248, 249, 250, 251,252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265,266, 267, 268, 269, 271, 272, 273, 292, 293, 294, 295, 296, 297, 298,299, 300, 301, 304, 305, 308, 309, 310, 311, 312, 313, 315, 316, 317,318, 319, 320, 321, 324, 325, 326, 327, 339, 340, 341, 342, 343, 344,345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 357, 361,363, 365, 367, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378,393, 394, 395, 397, 399, 400, 401, 402, 403, 405, 406, 408, 409, 410,411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 436,437, 440, 441, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473,474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 488, 489,490, 492, 493, 494, 495, 497, 498, 499, 500, 501, 502, 503, 504, 505,506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519,520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533,534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547,548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561,562, 563, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577,578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591,592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605,606, 607, 608, 609, 610, 611, 612, 613, 614, 615, 616, 617, 618, 619,620, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635,636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649,650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663,664, 665, 666, 667, 668, 669, 670, 671, 672, 677, 682, 683, 684, 685,686, 687, 688, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707,708, 717, 718, 731, 732, 733, 734, 735, 736, 737, 738, 740, 741, 742,743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 755, 756, 757,758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771,772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785,786, 787, 788, 789, 790, 791, 792, 793, 794, 795, 796, 797, 798, 799,800, 801, 802, 803, 804, 805, 806, 807, 808, 809, 818, 821, 823, 824,825, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VII)

In another aspect, the present invention provides compounds of Formula(VII)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (VII) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VII), X is N or CY¹. In another embodimentof Formula (VII), X is N. In another embodiment of Formula (VII), X isCY¹.

In one embodiment of Formula (VII), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VII), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VII), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VII), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VII), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VII), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VII), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (VII), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VII), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VII), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VII), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (VII), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VII), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VII), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VII), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VII), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VII), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (VII), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VII), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (VII), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VII), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VII), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (VII), R¹⁰ ateach occurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (VII), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VII), R¹¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VII)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that when X is CY¹ and Y¹ is hydrogen; and R³ isthiazolyl; the R³ thiazolyl is substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VII),which includes Examples 52, 55, 56, 61, 75, 77, 78, 79, 80, 81, 82, 83,85, 86, 87, 88, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102,103, 104, 105, 108, 114, 115, 116, 119, 120, 122, 123, 124, 125, 126,127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 139, 140, 141,142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155,156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169,170, 171, 172, 173, 175, 176, 177, 178, 179, 180, 183, 184, 186, 189,190, 191, 200, 201, 206, 215, 219, 240, 358, 359, 398, 462, 621, 622,676, 810, 820, 822, 831, 832, 833, 834, 835, 836, 842, 843, 844, 845,846, 847, 848, 849, 850, 851, 852, 853, and pharmaceutically acceptablesalts thereof.

Embodiments of Formula (VIII)

In another aspect, the present invention provides compounds of Formula(VIII)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (VIII) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIII), X is N or CY¹. In anotherembodiment of Formula (VIII), X is N. In another embodiment of Formula(VIII), X is CY¹.

In one embodiment of Formula (VIII), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIII), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIII), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VIII), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIII), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIII), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIII), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, C(O)R⁴,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and whereineach R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (VIII), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIII), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIII), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIII), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (VIII), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIII), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIII), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIII), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIII), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIII), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (VIII), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIII), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (VIII), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIII), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIII), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (VIII), R¹⁰ ateach occurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (VIII), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIII), R¹¹ at eachoccurrence, is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIII)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIII),which includes Example 322, and pharmaceutically acceptable saltsthereof.

Embodiments of Formula (IX)

In another aspect, the present invention provides compounds of Formula(IX)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (IX) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, alkyl, alkenyl, and alkynyl; and

R¹¹ at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent; and

when X is CY¹ and Y¹ is hydrogen; and R³ is phenyl; the R³ phenyl is notsubstituted at the para position with phenyl.

In one embodiment of Formula (IX), X is N or CY¹. In another embodimentof Formula (IX), X is N. In another embodiment of Formula (IX), X isCY¹.

In one embodiment of Formula (IX), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IX), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IX), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IX), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IX), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IX), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IX), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IX), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IX), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IX), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IX), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, and OH.

In another embodiment of Formula (IX), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IX), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IX), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹¹C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IX), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁶alkyl and alkenyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁹,OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IX), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IX), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IX), R⁸ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IX), R⁸ at each occurrence,is independently alkyl.

In one embodiment of Formula (IX), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IX), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IX), R¹⁰ at each occurrence, isindependently selected from the group consisting of haloalkyl, alkyl,alkenyl, and alkynyl. In another embodiment of Formula (IX), R¹⁰ at eachoccurrence, is independently haloalkyl or alkyl.

In one embodiment of Formula (IX), R¹¹ at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IX), R¹¹ at each occurrence,is independently alkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IX)

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, F, Cl, Br and I; wherein each R³ phenyl is optionallyadditionally substituted with one substituent independently selectedfrom the group consisting of F, Cl, Br and I; wherein each R³ 5-6membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl and 3-12 membered heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, OH,F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of R⁷, OR⁷, OH, F, Cl, Br and I;wherein each R⁵ aryl and heterocyclyl is optionally substituted withone, or two substituents independently selected from the groupconsisting of R⁸, OR⁸, CNF, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, and cycloalkyl;wherein each R⁶ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁹, OR⁹, SO₂R⁹, OH, F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, substituent independentlyselected from the group consisting of aryl, alkoxy, F, Cl, Br and I;wherein each R⁹ aryl, cycloalkyl, and heterocyclyl is optionallysubstituted with one, two, or three substituents independently selectedfrom the group consisting of R¹¹, OR¹¹, CO(O)R¹¹, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of haloalkyl, and alkyl; and

R¹¹ at each occurrence, is alkyl;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent; and

when X is CY¹ and Y¹ is hydrogen; and R³ is phenyl; the R³ phenyl is notsubstituted at the para position with phenyl.

Still another embodiment pertains to compounds having Formula (IX),which includes Examples 53, 54, 76, 314, 323, 491, and pharmaceuticallyacceptable salts thereof.

Embodiments of Formula (IA)

One embodiment, therefore, pertains to compounds or pharmaceuticallyacceptable salts thereof, which are useful as inhibitors of NAMPT, thecompounds having Formula (IA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

Z is CH, C—F, C—Cl, C—Br, C—I or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is hydrogen, F, Cl, Br, or I;

Z is CR²; and

R² is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R^(3x) is independently selected from the group consisting of phenyl andheterocyclyl; wherein each R^(3x) phenyl and heterocyclyl is substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴,OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂,NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH,C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I;

R¹¹ at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

m is 4, 5, or 6; and

n is 1 or 2;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is hydrogen; and R³is phenyl; the R³ phenyl is not substituted at the para position withphenyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

In one embodiment of Formula (IA), X is N or CY¹. In another embodimentof Formula (IA), X is N. In another embodiment of Formula (IA), X isCY¹.

In one embodiment of Formula (IA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IA), Z is CH, C—F, C—Cl, C—Br, C—I or N;and R¹ is independently selected from the group consisting ofNHC(O)NHR³, NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³,NHC(O)(CH₂)_(n)R³, C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x),C(O)NH(CH₂)_(m)R^(3x), CH₂C(O)NHR³, and CH₂NHC(O)R³. In anotherembodiment of Formula (IA), Z is CH or N; and R¹ is NHC(O)NHR³. Inanother embodiment of Formula (IA), Z is CH or N; and R¹ isNHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula (IA), Z is CHor N; and R¹ is CH₂NHC(O)NHR³. In another embodiment of Formula (IA), Zis CH or N; and R¹ is NHC(O)R³. In another embodiment of Formula (IA), Zis CH or N; and R¹ is NHC(O)(CH₂)_(n)R³. In another embodiment ofFormula (IA), Z is CH or N; and R¹ is C(O)NH(CH₂)_(n)R³. In anotherembodiment of Formula (IA), Z is CH or N; and R¹ isNHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IA), Z is CH orN; and R¹ is C(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IA), Z is CH or N; and R¹ is CH₂C(O)NHR³. In another embodiment ofFormula (IA), Z is CH or N; and R¹ is CH₂NHC(O)R³.

In one embodiment of Formula (IA), Z is CH; and R¹ is independentlyselected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IA), Zis CH; and R¹ is NHC(O)NHR³. In another embodiment of Formula (IA), Z isCH; and R¹ is NHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IA), Z is CH; and R¹ is CH₂NHC(O)NHR³. In another embodiment of Formula(IA), Z is CH; and R¹ is NHC(O)R³.

In another embodiment of Formula (IA), Z is CH; and R¹ isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (IA), Z is CH; andR¹ is C(O)NH(CH₂)_(n)R³. In another embodiment of Formula (IA), Z is CH;and R¹ is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IA),Z is CH; and R¹ is C(O)NH(CH₂)_(m)R^(3x). In another embodiment ofFormula (IA), Z is CH; and R¹ is CH₂C(O)NHR³. In another embodiment ofFormula (IA), Z is CH; and R¹ is CH₂NHC(O)R³.

In one embodiment of Formula (IA), Z is N; and R¹ is independentlyselected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IA), Zis N; and R¹ is NHC(O)NHR³. In another embodiment of Formula (IA), Z isN; and R¹ is NHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IA), Z is N; and R¹ is CH₂NHC(O)NHR³. In another embodiment of Formula(IA), Z is N; and R¹ is NHC(O)R³.

In another embodiment of Formula (IA), Z is N; and R¹ isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (IA), Z is N; and R¹is C(O)NH(CH₂)_(n)R³. In another embodiment of Formula (IA), Z is N; andR¹ is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IA), Z isN; and R¹ is C(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IA), Z is N; and R¹ is CH₂C(O)NHR³. In another embodiment of Formula(IA), Z is N; and R¹ is CH₂NHC(O)R³.

In one embodiment of Formula (IA), R¹ is hydrogen; Z is CR²; and R² isindependently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IA), R¹is hydrogen; Z is CR²; and R² is NHC(O)NHR³. In another embodiment ofFormula (IA), R¹ is hydrogen; Z is CR²; and R² isNHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula (IA), R¹ ishydrogen; Z is CR²; and R² is CH₂NHC(O)NHR³. In another embodiment ofFormula (IA), R¹ is hydrogen; Z is CR²; and R² is NHC(O)R³. In anotherembodiment of Formula (IA), R¹ is hydrogen; Z is CR²; and R² isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (IA), R¹ ishydrogen; Z is CR²; and R² is C(O)NH(CH₂)_(n)R³.

In another embodiment of Formula (IA), R¹ is hydrogen; Z is CR²; and R²is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IA), R¹ ishydrogen; Z is CR²; and R² is C(O)NH(CH₂)_(m)R^(3x). In anotherembodiment of Formula (IA), R¹ is hydrogen; Z is CR²; and R² isCH₂C(O)NHR³. In another embodiment of Formula (IA), R¹ is hydrogen; Z isCR²; and R² is CH₂NHC(O)R³.

In one embodiment of Formula (IA), m is 4, 5, or 6. In anotherembodiment of Formula (IA), m is 4. In another embodiment of Formula(IA), m is 5. In another embodiment of Formula (IA), m is 6.

In one embodiment of Formula (IA), n is 1 or 2. In another embodiment ofFormula (IA), n is 1. In another embodiment of Formula (IA), n is 2.

In one embodiment of Formula (IA), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IA), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, SO₂R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IA), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, SO₂R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IA), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IA), R^(3x) is independently selected fromthe group consisting of phenyl and heterocyclyl; wherein each R^(3x)phenyl and heterocycyl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴,N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴,NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IA), R^(3x) is heterocyclyl;wherein each R^(3x) heterocycyl is substituted with C(O)R⁴, or CO(O)R⁴.

In one embodiment of Formula (IA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)², NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, CN, F, and Cl.

In one embodiment of Formula (IA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IA), R¹⁰ at each occurrence, is independently heterocyclyl, cycloalkyl,alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionally substituted withone, two, three or four substituents independently selected from thegroup consisting of alkoxy, and F.

In one embodiment of Formula (IA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (IA), R¹¹, at each occurrence, is independentlyalkyl.

In another embodiment of Formula (IA), R¹¹, at each occurrence, isindependently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

Z is CH, C—F, or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, andCl;

R¹ is hydrogen;

Z is CR²; and

R² is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, CH₂C(O)NHR³, andCH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R^(3x) is heterocyclyl; wherein the R^(3x) heterocyclyl is substitutedwith one, two, three or four substituents independently selected fromthe group consisting of C(O)R⁴, CO(O)R⁴, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F;

R¹¹ at each occurrence, is independently cycloalkyl or alkyl;

m is 4, or 5; and

n is 1;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is hydrogen; and R³is phenyl; the R³ phenyl is not substituted at the para position withphenyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

Still another embodiment pertains to compounds having Formula (IA),which includes Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14,15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32,33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50,51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68,69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86,87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103,104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117,118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131,132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145,146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159,160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173,174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187,188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201,202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215,216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229,230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243,244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257,258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271,272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285,286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299,300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313,314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327,328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341,342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355,356, 357, 358, 359, 360, 361, 362, 363, 364, 365, 366, 367, 368, 369,370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383,384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397,398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411,412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425,426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439,440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453,454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467,468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481,482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495,496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509,510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523,524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537,538, 539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551,552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565,566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579,580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593,594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607,608, 609, 610, 611, 612, 613, 614, 615, 616, 617, 618, 619, 620, 621,622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635,636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649,650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663,664, 665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677,678, 679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691,692, 693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705,706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719,720, 721, 722, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733,734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747,748, 749, 750, 751, 752, 753, 754, 755, 756, 757, 758, 759, 760, 761,762, 763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773, 774, 775,776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789,790, 791, 792, 793, 794, 795, 796, 797, 798, 799, 800, 801, 802, 803,804, 805, 806, 807, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817,818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831,832, 833, 834, 835, 836, 837, 838, 839, 840, 841, 842, 843, 844, 845,846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859,860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 872, 873,874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887,888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901,902, 903, 904, 905, 906, 907, 908, 909, 910, 911, 912, 913, 914, 915,916, 917, 918, 919, 920, 921, 922, 923, 924, 925, 926, 927, 928, 929,930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943,944, 945, 946, 947, 948, 949, 950, 951, 952, 953, 954, 955, 956, 957,958, 959, 960, 961, 962, 963, 964, 965, 966, 967, 968, 969, 970, 971,972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985,986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999,1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011,1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1020, 1021, 1022, 1023,1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035,1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047,1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059,1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071,1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083,1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095,1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107,1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119,1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131,1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143,1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 437, 508,513, 516, 527, 529, 699, 915, 919, 923, 924, 925, 927, 934, 937, 985,996, 999, 1009, 1095, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIA)

In another aspect, the present invention provides compounds of Formula(IIA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IA).

One embodiment pertains to compounds of Formula (IIA) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IIA), X is N or CY¹. In another embodimentof Formula (IIA), X is N. In another embodiment of Formula (IIA), X isCY¹.

In one embodiment of Formula (IIA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IIA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IIA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IIA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IIA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IIA), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IIA), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IIA), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IIA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IIA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IIA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IIA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IIA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IIA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IIA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IIA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IIA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IIA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IIA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IIA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (IIA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (IIA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IIA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IIA),which includes Example 2; and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIIA)

In another aspect, the present invention provides compounds of Formula(IIIA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed in Formula (IA) herein.

One embodiment pertains to compounds of Formula (IIIA) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IIIA), X is N or CY¹. In anotherembodiment of Formula (IIIA), X is N. In another embodiment of Formula(IIIA), X is CY¹.

In one embodiment of Formula (IIIA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IIIA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IIIA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IIIA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IIIA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IIIA), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IIIA), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SO₂R⁴,C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; andwherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (IIIA), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IIIA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IIIA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IIIA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IIIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IIIA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IIIA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IIIA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IIIA), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (IIIA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IIIA), R⁸, at eachoccurrence, is independently alkyl.

In one embodiment of Formula (IIIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IIIA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IIIA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IIIA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (IIIA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (IIIA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IIIA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IIIA),which includes 1, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17,18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35,36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 89, 106,109, 110, 111, 112, 113, 396, and pharmaceutically acceptable saltsthereof.

Embodiments of Formula (IVA)

In another aspect, the present invention provides compounds of Formula(IVA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IA).

One embodiment pertains to compounds of Formula (IVA) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IVA), X is N or CY¹. In another embodimentof Formula (IVA), X is N. In another embodiment of Formula (IVA), X isCY¹.

In one embodiment of Formula (IVA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IVA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IVA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IVA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IVA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IVA), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IVA), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IVA), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IVA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IVA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IVA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IVA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IVA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IVA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IVA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IVA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IVA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IVA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IVA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IVA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IVA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IVA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IVA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IVA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (IVA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (IVA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IVA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IVA),which includes Examples 118, 216, 220, 221, 222, 223, 224, 225, 226,227, 228, 229, 243, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289,290, 291, 302, 303, 306, 307, 328, 329, 330, 331, 332, 333, 334, 335,336, 337, 338, 364, 366, 379, 380, 381, 382, 383, 384, 385, 386, 387,388, 389, 390, 391, 392, 404, 407, 424, 425, 426, 427, 428, 429, 430,431, 432, 433, 434, 435, 438, 439, 442, 443, 444, 445, 446, 447, 448,449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 486,487, 496, 564, 565, 673, 674, 675, 689, 690, 691, 692, 693, 694, 695,696, 709, 710, 711, 712, 713, 714, 715, 716, 719, 720, 721, 722, 723,724, 725, 726, 727, 728, 729, 730, 904, 912, 938, 939, 940, 941, 942,943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 953, 954, 955, 956,957, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1020, 1021,1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033,1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045,1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057,1058, 1059, 1060, 1065, 1066, 1069, 1070, 1071, 1072, 1073, 1074, 1075,1076, 1078, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130,1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142,1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, andpharmaceutically acceptable salts thereof.

Embodiments of Formula (VA)

In another aspect, the present invention provides compounds of Formula(VA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IA).

One embodiment pertains to compounds of Formula (VA) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VA), X is N or CY¹. In another embodimentof Formula (VA), X is N. In another embodiment of Formula (VA), X isCY¹.

In one embodiment of Formula (VA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VA), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VA), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VA), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (VA), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (VA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (VA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (VA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (VA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VA),which includes 59, 60, 274, 275, 276, 277, 278, 279, 360, 362, andpharmaceutically acceptable salts thereof.

Embodiments of Formula (VIA)

In another aspect, the present invention provides compounds of Formula(VIA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IA).

One embodiment pertains to compounds of Formula (VIA) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIA), X is N or CY¹. In another embodimentof Formula (VIA), X is N. In another embodiment of Formula (VIA), X isCY¹.

In one embodiment of Formula (VIA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VIA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIA), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIA), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (VIA), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (VIA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (VIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VIA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VIA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (VIA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (VIA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIA),which includes Examples 57, 117, 121, 138, 174, 181, 182, 185, 187, 188,192, 193, 194, 195, 196, 197, 198, 199, 202, 203, 204, 205, 207, 208,209, 210, 211, 212, 213, 214, 217, 218, 230, 231, 232, 233, 234, 235,236, 237, 238, 239, 241, 242, 244, 245, 246, 247, 248, 249, 250, 251,252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265,266, 267, 268, 269, 271, 272, 273, 292, 293, 294, 295, 296, 297, 298,299, 300, 301, 304, 305, 308, 309, 310, 311, 312, 313, 315, 316, 317,318, 319, 320, 321, 324, 325, 326, 327, 339, 340, 341, 342, 343, 344,345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 357, 361,363, 365, 367, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378,393, 394, 395, 397, 399, 400, 401, 402, 403, 405, 406, 408, 409, 410,411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 436,437, 440, 441, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473,474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 488, 489,490, 492, 493, 494, 495, 497, 498, 499, 500, 501, 502, 503, 504, 505,506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519,520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533,534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547,548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561,562, 563, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577,578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591,592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605,606, 607, 608, 609, 610, 611, 612, 613, 614, 615, 616, 617, 618, 619,620, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635,636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649,650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663,664, 665, 666, 667, 668, 669, 670, 671, 672, 677, 682, 683, 684, 685,686, 687, 688, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707,708, 717, 718, 731, 732, 733, 734, 735, 736, 737, 738, 740, 741, 742,743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 755, 756, 757,758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771,772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785,786, 787, 788, 789, 790, 791, 792, 793, 794, 795, 796, 797, 798, 799,800, 801, 802, 803, 804, 805, 806, 807, 808, 809, 818, 821, 823, 824,825, 857, 867, 868, 869, 870, 871, 872, 873, 874, 875, 876, 877, 878,879, 880, 881, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893,895, 896, 899, 906, 907, 909, 910, 913, 914, 915, 916, 917, 918, 919,920, 921, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933,934, 935, 936, 937, 958, 959, 960, 961, 962, 963, 964, 965, 966, 967,968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981,982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995,996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007,1008, 1009, 1010, 1061, 1062, 1063, 1064, 1068, 1077, 1082, 1083, 1084,1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096,1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108,1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120,and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIA)

In another aspect, the present invention provides compounds of Formula(VIIA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IA).

One embodiment pertains to compounds of Formula (VIIA) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIIA), X is N or CY¹. In anotherembodiment of Formula (VIIA), X is N. In another embodiment of Formula(VIIA), X is CY¹.

In one embodiment of Formula (VIIA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIIA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIIA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VIIA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIIA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIIA), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIIA), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SO₂R⁴,C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; andwherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (VIIA), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIIA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIIA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIIA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VIIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIIA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIIA), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (VIIA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIIA), R⁸, at eachoccurrence, is independently alkyl.

In one embodiment of Formula (VIIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIIA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VIIA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VIIA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (VIIA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (VIIA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIIA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIIA),which includes Examples 52, 55, 56, 61, 75, 77, 78, 79, 80, 81, 82, 83,85, 86, 87, 88, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102,103, 104, 105, 108, 114, 115, 116, 119, 120, 122, 123, 124, 125, 126,127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 139, 140, 141,142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155,156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169,170, 171, 172, 173, 175, 176, 177, 178, 179, 180, 183, 184, 186, 189,190, 191, 200, 201, 206, 215, 219, 240, 358, 359, 398, 462, 621, 622,676, 810, 820, 822, 831, 832, 833, 834, 835, 836, 842, 843, 844, 845,846, 847, 848, 849, 850, 851, 852, 853, 859, 860, 882, 898, andpharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIIA)

In another aspect, the present invention provides compounds of Formula(VIIIA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (VIIIA) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIIIA), X is N or CY¹. In anotherembodiment of Formula (VIIIA), X is N. In another embodiment of Formula(VIIIA), X is CY¹.

In one embodiment of Formula (VIIIA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIIIA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIIIA), X is CY¹; and Y¹ is Cl. In another embodiment ofFormula (VIIIA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIIIA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIIIA), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIIIA), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SO₂R⁴,C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; andwherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (VIIIA), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIIIA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIIIA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIIIA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VIIIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIIA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIIA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIIIA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIIA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIIIA), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (VIIIA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIIIA), R⁸, at eachoccurrence, is independently alkyl.

In one embodiment of Formula (VIIIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIIA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIIIA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VIIIA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VIIIA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (VIIIA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (VIIIA), R¹¹, at eachoccurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIIIA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIIIA),which includes Examples 322; and pharmaceutically acceptable saltsthereof.

Embodiments of Formula (IXA)

In another aspect, the present invention provides compounds of Formula(IXA)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (IX) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent; and

when X is CY¹ and Y¹ is hydrogen; and R³ is phenyl; the R³ phenyl is notsubstituted at the para position with phenyl.

In one embodiment of Formula (IXA), X is N or CY¹. In another embodimentof Formula (IXA), X is N. In another embodiment of Formula (IXA), X isCY¹.

In one embodiment of Formula (IXA), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IXA), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IXA), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IXA), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IXA), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IXA), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IXA), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IXA), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IXA), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IXA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IXA), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IXA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IXA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IXA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IXA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IXA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IXA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IXA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IXA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IXA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IXA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IXA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IXA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IXA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (IXA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (IXA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IXA)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent; and

when X is CY¹ and Y¹ is hydrogen; and R³ is phenyl; the R³ phenyl is notsubstituted at the para position with phenyl.

Still another embodiment pertains to compounds having Formula (IXA),which includes Examples 53, 54, 76, 314, 323, 491, and pharmaceuticallyacceptable salts thereof.

Embodiments of Formula (XA)

In another aspect, the present invention provides compounds of Formula(XA)

and pharmaceutically acceptable salts thereof; wherein R⁴ is asdescribed herein for Formula (IA).

One embodiment pertains to compounds of Formula (XA) or pharmaceuticallyacceptable salts thereof;

wherein

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I; and

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl.

In one embodiment of Formula (XA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (XA), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (XA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (XA), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (XA), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (XA), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (XA), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (XA), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (XA), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (XA), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (XA), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (XA), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (XA), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(XA), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (XA), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl. In anotherembodiment of Formula (XA), R¹¹, at each occurrence, is independentlyalkyl. In another embodiment of Formula (XA), R¹¹, at each occurrence,is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (XA)

wherein

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl.

Still another embodiment pertains to compounds having Formula (XA),which includes Examples 217, 230, 231, 232, 233, 234, 235, 236, 237,238, 239, 298, 301, 308, 309, 310, 311, 312, 313, 315, 367, 368, 369,370, 371, 372, 373, 374, 375, 376, 377, 378, 402, 437, 440, 441, 484,488, 490, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509,510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523,524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537,538, 539, 547, 548, 549, 550, 551, 552, 557, 562, 567, 568, 569, 580,581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594,595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608,609, 610, 611, 612, 613, 614, 615, 616, 617, 618, 619, 620, 623, 624,625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638,639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652,653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664, 665, 666,667, 668, 669, 670, 671, 672, 682, 683, 684, 699, 700, 701, 702, 703,704, 705, 706, 707, 708, 731, 732, 733, 737, 913, 914, 915, 916, 917,918, 919, 920, 921, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931,932, 933, 934, 935, 936, 937, 958, 959, 960, 961, 962, 963, 964, 965,966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979,980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993,994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006,1007, 1008, 1009, 1010, 1061, 1062, 1063, 1064, 1068, 1077, 1084, 1085,1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097,1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109,1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, andpharmaceutically acceptable salts thereof.

Embodiments of Formula (IB)

One embodiment, therefore, pertains to compounds or pharmaceuticallyacceptable salts thereof, which are useful as inhibitors of NAMPT, thecompounds having Formula (IB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

Z is CH, C—F, C—Cl, C—Br, C—I or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R¹ is hydrogen, F, Cl, Br, or I;

Z is CR²; and

R² is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R^(3x) is independently selected from the group consisting of phenyl andheterocyclyl; wherein each R^(3x) phenyl and heterocyclyl is substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴,OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂,NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH,C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I;

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂CHCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

m is 4, 5, or 6; and

n is 1 or 2;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

-   -   when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is        hydrogen; and R³ is phenyl; the R³ phenyl is not substituted at        the para position with phenyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

In one embodiment of Formula (IB), X is N or CY¹. In another embodimentof Formula (IB), X is N. In another embodiment of Formula (IB), X isCY¹.

In one embodiment of Formula (IB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IB), Z is CH, C—F, C—Cl, C—Br, C—I or N;and R is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IB), Zis CH or N; and R¹ is NHC(O)NHR³. In another embodiment of Formula (IB),Z is CH or N; and R¹ is NHC(O)NH(CH₂)_(m)R^(3x). In another embodimentof Formula (IB), Z is CH or N; and R¹ is CH₂NHC(O)NHR³. In anotherembodiment of Formula (IB), Z is CH or N; and R¹ is NHC(O)R³. In anotherembodiment of Formula (IB), Z is CH or N; and R¹ is NHC(O)(CH₂)_(n)R³.In another embodiment of Formula (IB), Z is CH or N; and R¹ isC(O)NH(CH₂)_(n)R³. In another embodiment of Formula (IB), Z is CH or N;and R¹ is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IB),Z is CH or N; and R¹ is C(O)NH(CH₂)_(m)R^(3x). In another embodiment ofFormula (IB), Z is CH or N; and R¹ is CH₂C(O)NHR³. In another embodimentof Formula (IB), Z is CH or N; and R¹ is CH₂NHC(O)R³.

In one embodiment of Formula (IB), Z is CH; and R¹ is independentlyselected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IB), Zis CH; and R¹ is NHC(O)NHR³. In another embodiment of Formula (IB), Z isCH; and R¹ is NHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IB), Z is CH; and R¹ is CH₂NHC(O)NHR³. In another embodiment of Formula(IB), Z is CH; and R¹ is NHC(O)R³.

In another embodiment of Formula (IB), Z is CH; and R¹ isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (IB), Z is CH; andR¹ is C(O)NH(CH₂)_(n)R³. In another embodiment of Formula (IB), Z is CH;and R¹ is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IB),Z is CH; and R¹ is C(O)NH(CH₂)_(m)R^(3x). In another embodiment ofFormula (IB), Z is CH; and R¹ is CH₂C(O)NHR³. In another embodiment ofFormula (IB), Z is CH; and R¹ is CH₂NHC(O)R³.

In one embodiment of Formula (IB), Z is N; and R¹ is independentlyselected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IB), Zis N; and R¹ is NHC(O)NHR³. In another embodiment of Formula (IB), Z isN; and R¹ is NHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IB), Z is N; and R¹ is CH₂NHC(O)NHR³. In another embodiment of Formula(IB), Z is N; and R¹ is NHC(O)R³.

In another embodiment of Formula (IB), Z is N; and R¹ isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (IB), Z is N; and R¹is C(O)NH(CH₂)_(n)R³. In another embodiment of Formula (IB), Z is N; andR¹ is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IB), Z isN; and R¹ is C(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula(IB), Z is N; and R¹ is CH₂C(O)NHR³. In another embodiment of Formula(IB), Z is N; and R¹ is CH₂NHC(O)R³.

In one embodiment of Formula (IB), R¹ is hydrogen; Z is CR²; and R² isindependently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³. In another embodiment of Formula (IB), R¹is hydrogen; Z is CR²; and R² is NHC(O)NHR³. In another embodiment ofFormula (IB), R¹ is hydrogen; Z is CR²; and R² isNHC(O)NH(CH₂)_(m)R^(3x). In another embodiment of Formula (IB), R¹ ishydrogen; Z is CR²; and R² is CH₂NHC(O)NHR³. In another embodiment ofFormula (IB), R¹ is hydrogen; Z is CR²; and R² is NHC(O)R³. In anotherembodiment of Formula (IB), R¹ is hydrogen; Z is CR²; and R² isNHC(O)(CH₂)_(n)R³. In another embodiment of Formula (IB), R¹ ishydrogen; Z is CR²; and R² is C(O)NH(CH₂)_(n)R³.

In another embodiment of Formula (IB), R¹ is hydrogen; Z is CR²; and R²is NHC(O)(CH₂)_(m)R^(3x). In another embodiment of Formula (IB), R¹ ishydrogen; Z is CR²; and R² is C(O)NH(CH₂)_(m)R^(3x). In anotherembodiment of Formula (IB), R¹ is hydrogen; Z is CR²; and R² isCH₂C(O)NHR³. In another embodiment of Formula (IB), R¹ is hydrogen; Z isCR²; and R² is CH₂NHC(O)R³.

In one embodiment of Formula (IB), m is 4, 5, or 6. In anotherembodiment of Formula (IB), m is 4. In another embodiment of Formula(IB), m is 5. In another embodiment of Formula (IB), m is 6.

In one embodiment of Formula (IB), n is 1 or 2. In another embodiment ofFormula (IB), n is 1. In another embodiment of Formula (IB), n is 2.

In one embodiment of Formula (IB), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IB), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, SO₂R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IB), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, SO₂R⁴, OR⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IB), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IB), R^(3x) is independently selected fromthe group consisting of phenyl and heterocyclyl; wherein each R^(3x)phenyl and heterocycyl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴,N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴,NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IB), R^(3x) is heterocyclyl;wherein each R^(3x) heterocycyl is substituted with C(O)R⁴, or CO(O)R⁴.

In one embodiment of Formula (IB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, CN, F, and Cl.

In one embodiment of Formula (IB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IB), R¹⁰ at each occurrence, is independently heterocyclyl, cycloalkyl,alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionally substituted withone, two, three or four substituents independently selected from thegroup consisting of alkoxy, and F.

In one embodiment of Formula (IB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (IB), R¹¹, at each occurrence, isindependently alkyl.

In another embodiment of Formula (IB), R¹¹, at each occurrence, isindependently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R¹ is independently selected from the group consisting of NHC(O)NHR³,NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³, NHC(O)(CH₂)_(n)R³,C(O)NH(CH₂)_(n)R³, NHC(O)(CH₂)_(m)R^(3x), C(O)NH(CH₂)_(m)R^(3x),CH₂C(O)NHR³, and CH₂NHC(O)R³; and

Z is CH, C—F, or N; or

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, andCl;

R¹ is hydrogen;

Z is CR²; and R² is independently selected from the group consisting ofNHC(O)NHR³, NHC(O)NH(CH₂)_(m)R^(3x), CH₂NHC(O)NHR³, NHC(O)R³,CH₂C(O)NHR³, and CH₂NHC(O)R³; and

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R^(3x) is heterocyclyl; wherein the R^(3x) heterocyclyl is substitutedwith one, two, three or four substituents independently selected fromthe group consisting of C(O)R⁴, CO(O)R⁴, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰ at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F;

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

m is 4, or 5; and

n is 1;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent;

when X is CY¹ and Y¹ is hydrogen; R¹ is NHC(O)R³; R² is hydrogen; and R³is phenyl; the R³ phenyl is not substituted at the para position withphenyl; when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is1; R² is hydrogen; and R³ is phenyl; the R³ phenyl is not substituted atthe para position with phenylmethoxy or 3-fluorophenoxy;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is furanyl; the R³ furanyl is not substituted withbenzyl, or 3-fluorophenyl methyl;

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is thienyl; the R³ thienyl is not substituted withphenoxy, 3-fluorophenoxy, or 3-chlorophenoxy; and

when X is CY¹ and Y¹ is hydrogen; R¹ is C(O)NH(CH₂)_(n)R³; n is 1; R² ishydrogen; and R³ is R³ phenyl; the phenyl is not substituted at the paraposition with SO₂R⁴ or SO₂NHR⁴.

Still another embodiment pertains to compounds having Formula (IB),which includes

-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-7-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenylethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(morpholin-4-yl)ethyl]benzamide;-   N-(1-hydroxy-2-methylpropan-2-yl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-benzyl-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-(cyclopentylmethyl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(piperidin-1-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenoxyethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(pyrrolidin-1-yl)ethyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(propan-2-yloxy)ethyl]benzamide;-   N-(2-hydroxy-2-methylpropyl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-[2-hydroxy-1-(4-methoxyphenyl)ethyl]-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(2-oxopyrrolidin-1-yl)ethyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydrofuran-2-ylmethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-propylbenzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(morpholin-4-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-phenylbenzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-methylbutyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(2-oxopyrrolidin-1-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydro-2H-pyran-4-ylmethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide;-   N-[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3,6-dihydropyridine-1    (2H)-carboxylate;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(tetrahydrofuran-3-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)urea;-   1-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   2-ethoxy-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(morpholin-4-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(2-methoxyethoxy)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3-methoxy-2-methylpropanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}butanamide;    4,4,4-trifluoro-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}butanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}tetrahydro-2H-pyran-4-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-4-methylpentanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-1-methylpiperidine-4-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}tetrahydro-2H-thiopyran-4-carboxamide    1,1-dioxide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-1,4-dioxane-2-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]butyl}piperidine-1-carboxylate;-   4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)benzamide;-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]butyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}urea;-   1-{4-[1-(cyclopentylcarbonyl)piperidin-4-yl]butyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]butyl}urea;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   2-cyclopentyl-N-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}acetamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(morpholin-4-ylacetyl)amino]benzamide;-   4-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenyl}-3,6-dihydropyridine-1    (2H)-carboxylate;-   N-{4-[(cyclopentylacetyl)amino]benzyl}imidazo[1,2-a]pyridine-6-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(3-phenylpyrrolidin-1-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-(1,3-dihydro-2H-isoindol-2-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[3-(tetrahydrofuran-2-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)butyl]-3-imidazo[1,2-a]pyridin-6-ylurea;-   2-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[2-oxo-4-(tetrahydrofuran-3-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;    2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(2-oxo-5-phenyl-1,3-oxazolidin-3-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methyl-1,3-thiazol-5-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methyl-1,3-thiazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(3-methyl-1,2-oxazol-5-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(3-chloro-1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(3-methoxy-1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(3,5-dimethyl-1,2-oxazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-{[3-(3,5-dimethyl-1,2-oxazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1-methyl-1H-pyrazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(4-methyl-1,3-thiazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-2-ylmethyl)(1H-tetrazol-5-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(1,2-oxazol-3-ylacetyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1,2-oxazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-2-ylmethyl)    [3-(1,3-thiazol-2-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydrofuran-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-3-ylmethyl)(tetrahydro-2H-pyran-4-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydrofuran-3-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-3-ylcarbonyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydro-2H-pyran-4-ylcarbonyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(3-methoxypropanoyl)[(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-3-ylcarbonyl)    [(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2R)-tetrahydrofuran-2-ylmethyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(3-methoxypropanoyl)    [(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-3-ylcarbonyl)    [(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2S)-tetrahydrofuran-2-ylmethyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydro-2H-pyran-4-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-({[2-(propan-2-yloxy)ethyl]carbamoyl}[(2R)-tetrahydrofuran-2-ylmethyl]amino)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl][(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-({[2-(propan-2-yloxy)ethyl]carbamoyl}[(2S)-tetrahydrofuran-2-ylmethyl]amino)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-[5-(4-chlorophenyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;    4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;    4-[(1-butanoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(3-methoxy-2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropanoyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(cyclohexylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2R)-2-hydroxybutyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(1-methyl-1H-pyrazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethyl-1H-pyrazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4S)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   2-{(4R)-4-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-{(4S)-4-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1-methyl-1H-pyrrol-2-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,5-dimethyl-1H-pyrazol-3-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-2-ylmethyl)(1,3-thiazol-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(1,2-oxazol-3-ylacetyl)[(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(5-methyl-1,2-oxazol-3-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1,2-oxazol-5-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1,2-oxazol-4-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(2R)-tetrahydrofuran-2-ylmethyl](1,3-thiazol-4-ylacetyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,5-dimethyl-1H-pyrazol-3-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1-methyl-1H-pyrazol-4-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(3,5-dimethyl-1,2-oxazol-4-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(1-methyl-1H-pyrazol-4-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1-methyl-1H-pyrrol-2-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   2-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   tert-butyl    {4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[3-(tetrahydrofuran-2-yl)propanoyl]amino}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide;    4-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(4-methylpentanoyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   4-[(4-cyanobenzyl)(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   2-{5-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   4-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   5-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]thiophene-2-carboxamide;-   1-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   2-[(2S)-2-(hydroxymethyl)-5-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4R)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   5-[1-(cyclopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]thiophene-2-carboxamide;-   2-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(5S)-2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(5R)-2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methoxyacetyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;    1-[4-(1-benzoylpiperidin-4-yl)butyl]-3-imidazo[1,2-a]pyridin-7-ylurea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(cyclohexylmethyl)-5-ethyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methoxy-3,3-dimethylcyclohexyl)methyl]-5-methyl-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide;-   3-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)propanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(propan-2-yloxy)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydrofuran-2-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-3-phenylpropanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide;-   3-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)propanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(propan-2-yloxy)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydrofuran-2-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3-phenylpropanamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   tert-butyl    4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylate;-   tert-butyl    (3R)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylate;-   tert-butyl    {2-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(morpholin-4-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-(1-ethyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(1,1-dioxidotetrahydrothiophen-3-yl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-phenylthiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(methylsulfonyl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}pyrrolidine-1-carboxylate;-   tert-butyl    3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)pyrrolidine-1-carboxylate;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)biphenyl-2-sulfonamide;-   5-{1-[(2R)-2-hydroxypropyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[(cyclopentylacetyl)amino]-3-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-{2-fluoro-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   4-[1-(cyclopropylacetyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   tert-butyl    4-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}-3,6-dihydropyridine-1    (2H)-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(propan-2-yloxy)phenyl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   tert-butyl    4-[4-(imidazo[1,2-a]pyridin-7-ylcarbamoyl)phenyl]piperidine-1-carboxylate;-   tert-butyl    4-[4-(imidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl]piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(2-methylpropanoyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   5-[3-(benzoylamino)oxetan-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(tetrahydrofuran-3-ylacetyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(pentanoylamino)oxetan-3-yl]thiophene-2-carboxamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(4-{[(3R)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(4-{[(3R)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3R)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}benzamide;-   5-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-3-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(3-methoxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-butanoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(3-hydroxy-3-methylbutanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2-(4-benzoylpiperazin-1-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(propan-2-yl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-phenyl-1,3-thiazole-5-carboxamide;-   1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide;-   tert-butyl    3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)azetidine-1-carboxylate;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]benzamide;-   1-[4-(1-acetylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}phenyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4-ylacetyl)pyrrolidin-3-yl]phenyl}urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   4-{[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]amino}-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-6-yl)methyl]-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   5-(4-hydroxytetrahydro-2H-pyran-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}azetidine-1-carboxylate;-   tert-butyl    4-hydroxy-4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[5-(piperidin-1-ylcarbonyl)-1,3-thiazol-2-yl]urea;-   5-{3-hydroxy-1-[(2S)-2-methylbutanoyl]azetidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(3-{[(2S)-2-methylbutanoyl]amino}oxetan-3-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1-[1-(3-methylbutanoyl)piperidin-4-yl]-1H-pyrazole-3-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   1-{4-[(1-acetylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[(1-benzoylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(propan-2-yloxy)acetyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(4-{[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)urea;-   1-(4-{[1-(1,4-dioxan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)urea;-   tert-butyl    (3R)-3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}pyrrolidine-1-carboxylate;-   4-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-{1-[(3,3-difluorocyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[(1-benzoylpiperidin-4-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)azetidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylazetidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(propan-2-yloxy)acetyl]azetidin-3-yl}phenyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]phenyl}urea;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[6-(morpholin-4-yl)pyridin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methyltetrahydro-2H-pyran-2-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylbutanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-{[(2S)-2-methylbutanoyl]amino}cyclobutyl)thiophene-2-carboxamide;-   5-[1-(benzoylamino)cyclobutyl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3,3,3-trifluoropropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(1-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}cyclobutyl)tetrahydro-2H-pyran-4-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}azetidine-1-carboxylate;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   4-[1-(furan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(piperidin-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-phenoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)azetidin-3-yl]benzamide;-   tert-butyl    4-{4-[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-phenoxyphenyl)urea;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2,2-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohexylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   4-(1-butanoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylpent-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyloxetan-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopropyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopentylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-oxobutanoyl)piperidin-4-yl]benzamide;-   4-{1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-propanoylpiperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(2,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;    4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)azetidin-3-yl]benzamide;-   5-[4-hydroxy-1-(3-methylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[4-hydroxy-1-(2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-4-hydroxypiperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylazetidin-3-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   tert-butyl    4-{4-[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   2-cyclopentyl-N-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   tert-butyl    4-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-1-ylcarbonyl)benzamide;-   4-[1-(ethylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)azetidin-3-yl]benzamide;-   propan-2-yl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   2-methylpropyl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(2-cyano-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3R)-tetrahydrofuran-3-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}benzamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(ethylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)azetidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)azetidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)azetidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)pyrrolidin-3-yl]benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide;-   4-[1-(cyclopropylsulfonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-{(1R)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{(1R)-3-methyl-1-[(tetrahydrofuran-3-ylacetyl)amino]butyl}thiophene-2-carboxamide;-   5-{(1S)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1-phenylpiperidin-4-yl)-1,3-thiazole-5-carboxamide;-   1-(4-{[(3R)-1-(2-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(3-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(4-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(4-{[(3R)-1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(2-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(4-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(pyridin-2-yl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   1-[4-(1-butanoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopropyl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(phenylacetyl)piperidin-4-yl]phenyl}urea;-   5-[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4-methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   1-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3-fluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(2,4-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(2,5-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3,4-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3,5-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methyl-2-phenylpropanoyl)pyrrolidin-3-yl]benzamide;-   4-{1-[difluoro(phenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]furan-2-carboxamide;-   4-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   5-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[4-(2-methylpropyl)phenyl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-2-methylbutanoyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{1-[(2-methylpropyl)sulfonyl]pyrrolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(phenylsulfonyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidine-1-carboxylate;-   5-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-{1-[(3-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(3,5-difluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2E)-2-methylpent-2-enoyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-{1-[(2,5-dimethylfuran-3-yl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propanoylpyrrolidin-3-yl)thiophene-2-carboxamide;-   5-{1-[(1-cyanocyclopropyl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-butanoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyrazin-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(phenylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   2-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   5-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   2-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-[2-(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)ethyl]piperazine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutyl)-1H-pyrazol-5-yl]furan-2-carboxamide;-   5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(3-methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-methylbutanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(1-methylpiperidin-4-yl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}acetamide;-   tert-butyl    4-{4-[(imidazo[1,2-b]pyridazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-b]pyridazin-6-ylmethyl)benzamide;-   5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(propan-2-ylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(phenylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}piperidine-1-carboxylate;-   N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide;-   2-(imidazo[1,2-a]pyridin-6-yl)-N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}acetamide;-   N-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2-methoxyphenyl)acetyl]amino}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(phenylacetyl)amino]benzamide;-   4-(benzoylamino)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   3,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   3,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   2,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   2-fluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-3-methoxybenzamide;-   4-{[(2-fluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-methyl-2-(piperazin-1-yl)propanoyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-2-methoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(phenylsulfonyl)benzamide;-   4-(phenylsulfonyl)-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)benzamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-oxatricyclo[3.3.1.1˜3,7˜]dec-1-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   4-{[(2,5-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(2,4-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-cyclopropyl-1-(2-methoxyethyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   4-{[difluoro(phenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(2-methyl-2-phenylpropanoyl)amino]benzamide;-   N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(phenylsulfonyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(phenylsulfonyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylate;-   N-[(3-chloroimidazo[1,2-a]pyrazin-6-yl)methyl]-4-[(cyclopentylacetyl)amino]benzamide;-   N-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   2-(imidazo[1,2-a]pyridin-7-yl)-N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}acetamide;-   1-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-methyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide;-   5-[1-benzyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   N-(2,5-difluorobenzyl)-N′-(imidazo[1,2-a]pyridin-7-ylmethyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(propan-2-yl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-{4-[5-(2,2-dimethylpropyl)-1,3,4-oxadiazol-2-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   tert-butyl    4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbut-2-enoyl)piperidin-4-yl]benzamide;-   4-[1-(3-fluoro-4-methoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopent-1-en-1-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-ethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxyphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2-acetylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(methoxymethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-phenylpropanoyl)piperidin-4-yl]benzamide;-   4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[(2-methylpropyl)sulfonyl]acetyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-phenoxypropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-({[(1R,2S)-2-methylcyclohexyl]oxy}acetyl)piperidin-4-yl]benzamide;-   4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methoxyphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylbut-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5-methylphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-(4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3-methylbut-2-enoyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopent-1-en-1-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2-ethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,4-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,5-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-oxo-2,3-dihydro-1H-inden-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-2-methylbut-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(1H-indol-3-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-4,5,6,7-tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(pyridin-2-yl)cyclopropyl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-dihydro-2H-chromen-6-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(cyclohexyloxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloropyridin-3-yl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-cyclopropyl-1,2-oxazol-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2H-chromen-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-1,3-benzoxazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thieno[3,2-b]pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinolin-7-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(5,6,7,8-tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-7-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinoxalin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(2-methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(pyridin-2-yl)prop-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(8-methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methyl-4H-furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-8-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[3-methyl-1-(prop-2-en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)benzamide;-   4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)tetrahydro-2H-pyran-4-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxy-6-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(4-{1-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-4,5,6,7-tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(pyridin-2-yl)cyclopropyl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,3-dihydro-1-benzofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-1,3-benzoxazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(cinnolin-4-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinolin-7-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(5,6,7,8-tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-7-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinoxalin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(2-methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(pyridin-2-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-2,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(8-methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methyl-4H-furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2,3-dihydro-1-benzofuran-5-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-1-ethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-8-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[3-methyl-1-(prop-2-en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-{4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-methyl-5-(propan-2-yl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide;-   1-(4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   tert-butyl    4-{3-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]benzamide;-   1-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(4-methylpentanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(2-fluoro-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2-cyanobenzoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-N,N-dimethylpiperidine-1-carboxamide;-   1-{2-fluoro-4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   4-[(cyclopentylacetyl)amino]-N-[(7-fluoroimidazo[1,2-a]pyridin-6-yl)methyl]benzamide;-   N-[(7-fluoroimidazo[1,2-a]pyridin-6-yl)methyl]-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-2-(imidazo[1,2-a]pyridin-7-yl)acetamide;-   5-{1-[2,2-dimethyl-3-(piperazin-1-yl)propyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-amino-2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]acetyl}piperidin-4-yl)benzamide;-   4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-1-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxy-5-methylpyridin-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[4-(propan-2-yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-5-propyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2,3-dihydro-1-benzofuran-7-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3-thiazol-4-yl]carbonyl}piperidin-4-yl)benzamide;-   4-(1-{[1-(difluoromethyl)-5-methyl-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazolo[1,5-a]pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3-oxazol-4-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5-methylpyridin-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide;-   1-(4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(thieno[3,2-b]furan-5-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxy-5-methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[4-(propan-2-yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-5-propyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(pyrazolo[1,5-a]pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(propan-2-yl)-1,3-oxazol-4-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-7-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxy-5-methylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H-indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H-indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[6-(trifluoromethyl)pyrimidin-4-yl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   5-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   4-(1-benzoylpiperidin-4-yl)-2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide;-   2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-({4-methyl-1-[2-(piperazin-1-yl)ethyl]piperidin-4-yl}methyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   S-(2-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-2-oxoethyl)-L-cysteine;-   5-(1-{[1-(15-amino-4,7,10,13-tetraoxapentadecan-1-oyl)-4-methylpiperidin-4-yl]methyl}-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   S-{2-[(3-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-3-oxopropyl)amino]-2-oxoethyl}-L-cysteine;    and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds of Formula (IB) selectedfrom the group consisting of

-   4-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluoro-4-methoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2-acetylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(methoxymethyl)benzoyl]piperidin-4-yl}benzamide;-   4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxy-6-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIB)

In another aspect, the present invention provides compounds of Formula(IIB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IB).

One embodiment pertains to compounds of Formula (IIB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IIB), X is N or CY¹. In another embodimentof Formula (IIB), X is N. In another embodiment of Formula (IIB), X isCY¹.

In one embodiment of Formula (IIB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IIB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IIB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IIB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IIB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IIB), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IIB), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IIB), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IIB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IIB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IIB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IIB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IIB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IIB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IIB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IIB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IIB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IIB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IIB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IIB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (IIB), R¹¹, at each occurrence, isindependently alkyl. In another embodiment of Formula (IIB), R¹¹, ateach occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IIB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IIB),which include

-   4-[(imidazo[1,2-a]pyridin-7-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide;    and    pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIIB)

In another aspect, the present invention provides compounds of Formula(IIIB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed in Formula (IB) herein.

One embodiment pertains to compounds of Formula (IIIB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IIIB), X is N or CY¹. In anotherembodiment of Formula (IIIB), X is N. In another embodiment of Formula(IIIB), X is CY¹.

In one embodiment of Formula (IIIB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IIIB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IIIB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IIIB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IIIB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IIIB), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IIIB), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SO₂R⁴,C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; andwherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (IIIB), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IIIB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IIIB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IIIB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IIIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IIIB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IIIB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IIIB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IIIB), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (IIIB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IIIB), R⁸, at eachoccurrence, is independently alkyl.

In one embodiment of Formula (IIIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IIIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IIIB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IIIB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IIIB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (IIIB), R¹¹, at each occurrence, isindependently alkyl. In another embodiment of Formula (IIIB), R¹¹, ateach occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IIIB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IIIB),which include

-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide;-   2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenylethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(morpholin-4-yl)ethyl]benzamide;-   N-(1-hydroxy-2-methylpropan-2-yl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-benzyl-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-(cyclopentylmethyl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(piperidin-1-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenoxyethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(pyrrolidin-1-yl)ethyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(propan-2-yloxy)ethyl]benzamide;-   N-(2-hydroxy-2-methylpropyl)-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   N-[2-hydroxy-1-(4-methoxyphenyl)ethyl]-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[2-(2-oxopyrrolidin-1-yl)ethyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydrofuran-2-ylmethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-propylbenzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(morpholin-4-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-phenylbenzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-methylbutyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-[3-(2-oxopyrrolidin-1-yl)propyl]benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydro-2H-pyran-4-ylmethyl)benzamide;-   4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide;-   N-[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]-4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3,6-dihydropyridine-1    (2H)-carboxylate;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(tetrahydrofuran-3-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)urea;-   1-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea;-   2-ethoxy-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(morpholin-4-yl)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-2-(2-methoxyethoxy)acetamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3-methoxy-2-methylpropanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}butanamide;-   4,4,4-trifluoro-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}butanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}tetrahydro-2H-pyran-4-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-4-methylpentanamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-1-methylpiperidine-4-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}tetrahydro-2H-thiopyran-4-carboxamide    1,1-dioxide;-   N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-1,4-dioxane-2-carboxamide;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}piperidine-1-carboxylate;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-imidazo[1,2-a]pyridin-6-ylurea;-   1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   4-{[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]amino}-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IVB)

In another aspect, the present invention provides compounds of Formula(IVB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IB).

One embodiment pertains to compounds of Formula (IVB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (IVB), X is N or CY¹. In another embodimentof Formula (IVB), X is N. In another embodiment of Formula (IVB), X isCY¹.

In one embodiment of Formula (IVB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IVB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IVB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IVB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IVB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IVB), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IVB), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IVB), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IVB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IVB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IVB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IVB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IVB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IVB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IVB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IVB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IVB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IVB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IVB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IVB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IVB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IVB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IVB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IVB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂CHCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (IVB), R¹¹, at each occurrence, isindependently alkyl. In another embodiment of Formula (IVB), R¹¹, ateach occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IVB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (IVB),which include

-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   1-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide;-   3-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)propanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(propan-2-yloxy)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydrofuran-2-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3-phenylpropanamide;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea;-   tert-butyl    4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylate;-   tert-butyl    (3R)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylate;-   tert-butyl    3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)pyrrolidine-1-carboxylate;-   N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)biphenyl-2-sulfonamide;-   1-{2-fluoro-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(4-{[(3R)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(4-{[(3R)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}phenyl)urea;-   tert-butyl    3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)azetidine-1-carboxylate;-   tert-butyl    4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)piperidine-1-carboxylate;-   1-[4-(1-acetylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethylpropanoyl)pyrrolidin-3-{4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}phenyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]phenyl}urea;-   1-{4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4-ylacetyl)pyrrolidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[5-(piperidin-1-ylcarbonyl)-1,3-thiazol-2-yl]urea;-   2-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)-1,3-thiazole-5-carboxamide;-   1-{4-[(1-acetylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[(1-benzoylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(propan-2-yloxy)acetyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(4-{[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)urea;-   1-(4-{[1-(1,4-dioxan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)urea;-   1-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[(1-benzoylpiperidin-4-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)azetidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylazetidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(propan-2-yloxy)acetyl]azetidin-3-yl}phenyl)urea;-   1-{4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]azetidin-3-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-phenoxyphenyl)urea;-   2-cyclopentyl-N-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   tert-butyl    4-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea;-   1-(4-{[(3R)-1-(2-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(3-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(4-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}oxy)phenyl]urea;-   1-(4-{[(3R)-1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(2-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[(3R)-1-(4-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-butanoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopropyl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(cyclopropylacetyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(phenylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3-fluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(2,4-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(2,5-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3,4-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{[1-(3,5-difluorobenzoyl)piperidin-4-yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea;-   tert-butyl    4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate;-   1-(4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3-methylbut-2-enoyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopent-1-en-1-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2-ethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,4-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,5-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-oxo-2,3-dihydro-1H-inden-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-2-methylbut-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(1H-indol-3-ylacetyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(4-{1-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-4,5,6,7-tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(pyridin-2-yl)cyclopropyl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,3-dihydro-1-benzofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-4-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-1,3-benzoxazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(cinnolin-4-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinolin-7-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(5,6,7,8-tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-7-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinoxalin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(2-methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(pyridin-2-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-2,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(8-methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methyl-4H-furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2,3-dihydro-1-benzofuran-5-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-1-ethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-8-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-{4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[3-methyl-1-(prop-2-en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-{4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(4-methylpentanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(2-fluoro-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(2-cyanobenzoyl)piperidin-4-yl]-2-fluorophenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{2-fluoro-4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(thieno[3,2-b]furan-5-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-[4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-{4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxy-5-methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[4-(propan-2-yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-5-propyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(pyrazolo[1,5-a]pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea;-   1-{4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(propan-2-yl)-1,3-oxazol-4-yl]carbonyl}piperidin-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-7-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxy-5-methylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H-indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H-indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H-indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea;-   1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)phenyl]urea;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VB)

In another aspect, the present invention provides compounds of Formula(VB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IB).

One embodiment pertains to compounds of Formula (VB) or pharmaceuticallyacceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R)₂, C(O)NH₂,C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸,SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸,C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VB), X is N or CY¹. In another embodimentof Formula (VB), X is N. In another embodiment of Formula (VB), X isCY¹.

In one embodiment of Formula (VB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VB), R³ is independently selected from thegroup consisting of phenyl and 5-6 membered heteroaryl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VB), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VB), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (VB), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (VB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (VB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (VB), R¹¹, at each occurrence, isindependently alkyl. In another embodiment of Formula (VB), R¹¹, at eachoccurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VB),which include

-   4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)benzamide;-   2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide;-   3-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)propanamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(propan-2-yloxy)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydrofuran-2-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-2-(tetrahydro-2H-pyran-4-yl)acetamide;-   N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-3-phenylpropanamide;-   1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea;-   1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIB)

In another aspect, the present invention provides compounds of Formula(VIB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IB).

One embodiment pertains to compounds of Formula (VIB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIB), X is N or CY¹. In another embodimentof Formula (VIB), X is N. In another embodiment of Formula (VIB), X isCY¹.

In one embodiment of Formula (VIB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VIB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIB), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIB), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (VIB), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (VIB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (VIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VIB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VIB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂CHCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH. In another embodiment of Formula (VIB), R¹¹, ateach occurrence, is independently alkyl. In another embodiment ofFormula (VIB), R¹¹, at each occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIB),which include

-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4S)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   2-{(4R)-4-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-{(4S)-4-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(1,2-oxazol-3-ylacetyl)[(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(5-methyl-1,2-oxazol-3-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1,2-oxazol-5-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1,2-oxazol-4-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(2R)-tetrahydrofuran-2-ylmethyl](1,3-thiazol-4-ylacetyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,5-dimethyl-1H-pyrazol-3-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1-methyl-1H-pyrazol-4-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(3,5-dimethyl-1,2-oxazol-4-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[(1-methyl-1H-pyrazol-4-yl)acetyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{[3-(1-methyl-1H-pyrrol-2-yl)propanoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   2-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-1,3-thiazole-5-carboxamide;-   tert-butyl    {4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[3-(tetrahydrofuran-2-yl)propanoyl]amino}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide;-   4-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(4-methylpentanoyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   2-{5-[(benzyloxy)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   5-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]thiophene-2-carboxamide;-   2-[(2S)-2-(hydroxymethyl)-5-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[(4R)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   5-[1-(cyclopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]thiophene-2-carboxamide;-   2-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(5S)-2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{(5R)-2-oxo-5-[(propan-2-yloxy)methyl]-1,3-oxazolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methoxyacetyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-[1-(cyclohexylmethyl)-5-ethyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methoxy-3,3-dimethylcyclohexyl)methyl]-5-methyl-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    {2-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(morpholin-4-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-(1-ethyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(1,1-dioxidotetrahydrothiophen-3-yl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   2-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-phenylthiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(methylsulfonyl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}pyrrolidine-1-carboxylate;-   5-{1-[(2R)-2-hydroxypropyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[(cyclopentylacetyl)amino]-3-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   4-[1-(cyclopropylacetyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(propan-2-yloxy)phenyl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(2-methylpropanoyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   5-[3-(benzoylamino)oxetan-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(tetrahydrofuran-3-ylacetyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(pentanoylamino)oxetan-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3R)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}benzamide;-   5-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-3-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(3-methoxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-butanoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(3-hydroxy-3-methylbutanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2-(4-benzoylpiperazin-1-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(propan-2-yl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-phenyl-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-(4-hydroxytetrahydro-2H-pyran-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}azetidine-1-carboxylate;-   tert-butyl    4-hydroxy-4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   5-{3-hydroxy-1-[(2S)-2-methylbutanoyl]azetidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(3-{[(2S)-2-methylbutanoyl]amino}oxetan-3-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1-[1-(3-methylbutanoyl)piperidin-4-yl]-1H-pyrazole-3-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   tert-butyl    (3R)-3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}pyrrolidine-1-carboxylate;-   4-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3,3-difluorocyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[6-(morpholin-4-yl)pyridin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methyltetrahydro-2H-pyran-2-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylbutanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-{[(2S)-2-methylbutanoyl]amino}cyclobutyl)thiophene-2-carboxamide;-   5-[1-(benzoylamino)cyclobutyl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3,3,3-trifluoropropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(1-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}cyclobutyl)tetrahydro-2H-pyran-4-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}azetidine-1-carboxylate;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   4-[1-(furan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(piperidin-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-phenoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2,2-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohexylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   4-(1-butanoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylpent-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyloxetan-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopropyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopentylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-oxobutanoyl)piperidin-4-yl]benzamide;-   4-{1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-propanoylpiperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(2,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)azetidin-3-yl]benzamide;-   5-[4-hydroxy-1-(3-methylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[4-hydroxy-1-(2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-4-hydroxypiperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylazetidin-3-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   tert-butyl    4-{4-[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-1-ylcarbonyl)benzamide;-   4-[1-(ethylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)azetidin-3-yl]benzamide;-   propan-2-yl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   2-methylpropyl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(2-cyano-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3R)-tetrahydrofuran-3-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(ethylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)azetidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)azetidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)azetidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)pyrrolidin-3-yl]benzamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide;-   4-[1-(cyclopropylsulfonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-{(1R)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{(1R)-3-methyl-1-[(tetrahydrofuran-3-ylacetyl)amino]butyl}thiophene-2-carboxamide;-   5-{(1S)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1-phenylpiperidin-4-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(pyridin-2-yl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   5-[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4-methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methyl-2-phenylpropanoyl)pyrrolidin-3-yl]benzamide;-   4-{1-[difluoro(phenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]furan-2-carboxamide;-   4-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   5-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[4-(2-methylpropyl)phenyl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-2-methylbutanoyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{1-[(2-methylpropyl)sulfonyl]pyrrolidin-3-yl}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(phenylsulfonyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidine-1-carboxylate;-   5-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-{1-[(3-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(3,5-difluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2E)-2-methylpent-2-enoyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-{1-[(2,5-dimethylfuran-3-yl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propanoylpyrrolidin-3-yl)thiophene-2-carboxamide;-   5-{1-[(1-cyanocyclopropyl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-butanoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyrazin-2-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]pyrrolidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide;-   5-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(phenylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide;-   2-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   5-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   2-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-[2-(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)ethyl]piperazine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutyl)-1H-pyrazol-5-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2-methoxyphenyl)acetyl]amino}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(phenylacetyl)amino]benzamide;-   4-(benzoylamino)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   3,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   3,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   2,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   2-fluoro-N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}benzamide;-   N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-3-methoxybenzamide;-   4-{[(2-fluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-methyl-2-(piperazin-1-yl)propanoyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-2-methoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(phenylsulfonyl)benzamide;-   5-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-oxatricyclo[3.3.1.1˜3,7˜]dec-1-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   4-{[(2,5-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(2,4-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-cycloproopyl-1-(2-methoxyethyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-{[difluoro(phenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(2-methyl-2-phenylpropanoyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-methyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide;-   5-[1-benzyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(2,5-difluorobenzyl)-N′-(imidazo[1,2-a]pyridin-7-ylmethyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(propan-2-yl)pyrrolidin-1-yl]carbonyl}benzamide;-   4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbut-2-enoyl)piperidin-4-yl]benzamide;-   4-[1-(3-fluoro-4-methoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopent-1-en-1-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-ethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxyphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2-acetylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(methoxymethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-phenylpropanoyl)piperidin-4-yl]benzamide;-   4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[(2-methylpropyl)sulfonyl]acetyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-phenoxypropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-({[(1R,2S)-2-methylcyclohexyl]oxy}acetyl)piperidin-4-yl]benzamide;-   4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methoxyphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylbut-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5-methylphenyl)acetyl]piperidin-4-yl}benzamide;-   4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-4,5,6,7-tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(pyridin-2-yl)cyclopropyl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-dihydro-2H-chromen-6-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(cyclohexyloxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloropyridin-3-yl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-cyclopropyl-1,2-oxazol-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2H-chromen-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-1,3-benzoxazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thieno[3,2-b]pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinolin-7-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(5,6,7,8-tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-7-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinoxalin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(2-methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(pyridin-2-yl)prop-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(8-methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methyl-4H-furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-8-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[3-methyl-1-(prop-2-en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)benzamide;-   4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)benzamide;-   4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)tetrahydro-2H-pyran-4-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxy-6-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-methyl-5-(propan-2-yl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]benzamide;-   4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-N,N-dimethylpiperidine-1-carboxamide;-   5-{1-[2,2-dimethyl-3-(piperazin-1-yl)propyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-amino-2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxythiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-pyrazol-3-yl]acetyl}piperidin-4-yl)benzamide;-   4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-1-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxy-5-methylpyridin-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[4-(propan-2-yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-5-propyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2,3-dihydro-1-benzofuran-7-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3-thiazol-4-yl]carbonyl}piperidin-4-yl)benzamide;-   4-(1-{[1-(difluoromethyl)-5-methyl-1H-pyrazol-3-yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazolo[1,5-a]pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3-oxazol-4-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5-methylpyridin-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-6-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[6-(trifluoromethyl)pyrimidin-4-yl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   5-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-({4-methyl-1-[2-(piperazin-1-yl)ethyl]piperidin-4-yl}methyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   S-(2-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-2-oxoethyl)-L-cysteine;-   5-(1-{[1-(15-amino-4,7,10,13-tetraoxapentadecan-1-oyl)-4-methylpiperidin-4-yl]methyl}-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   S-{2-[(3-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-3-oxopropyl)amino]-2-oxoethyl}-L-cysteine;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIB)

In another aspect, the present invention provides compounds of Formula(VIIB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (IB).

One embodiment pertains to compounds of Formula (VIIB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂CHCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIIB), X is N or CY¹. In anotherembodiment of Formula (VIIB), X is N. In another embodiment of Formula(VIIB), X is CY¹.

In one embodiment of Formula (VIIB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIIB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIIB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(VIIB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIIB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIIB), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIIB), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SO₂R⁴,C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; andwherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (VIIB), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIIB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIIB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIIB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VIIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIIB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIIB), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (VIIB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIIB), R⁸, at eachoccurrence, is independently alkyl.

In one embodiment of Formula (VIIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIIB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VIIB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VIIB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (VIIB), R¹¹, at each occurrence, isindependently alkyl. In another embodiment of Formula (VIIB), R¹¹, ateach occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIIB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIIB),which include

-   4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(morpholin-4-ylacetyl)amino]benzamide;-   4-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenyl}-3,6-dihydropyridine-1    (2H)-carboxylate;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(3-phenylpyrrolidin-1-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-(1,3-dihydro-2H-isoindol-2-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[3-(tetrahydrofuran-2-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;-   4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   2-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[2-oxo-4-(tetrahydrofuran-3-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(2-oxo-5-phenyl-1,3-oxazolidin-3-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methyl-1,3-thiazol-5-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methyl-1,3-thiazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(3-methyl-1,2-oxazol-5-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(3-chloro-1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(3-methoxy-1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(3,5-dimethyl-1,2-oxazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   2-{[3-(3,5-dimethyl-1,2-oxazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1-methyl-1H-pyrazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(4-methyl-1,3-thiazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-2-ylmethyl)(1H-tetrazol-5-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1,2-oxazol-5-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(1,2-oxazol-3-ylacetyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1,2-oxazol-4-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-2-ylmethyl)    [3-(1,3-thiazol-2-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydrofuran-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-3-ylmethyl)(tetrahydro-2H-pyran-4-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydrofuran-3-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-3-ylcarbonyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydro-2H-pyran-4-ylcarbonyl)(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(3-methoxypropanoyl)[(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-3-ylcarbonyl)    [(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2R)-tetrahydrofuran-2-ylmethyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(3-methoxypropanoyl)[(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{(tetrahydrofuran-3-ylcarbonyl)    [(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2S)-tetrahydrofuran-2-ylmethyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl](tetrahydro-2H-pyran-4-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydro-2H-pyran-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl][(2R)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-({[2-(propan-2-yloxy)ethyl]carbamoyl}[(2R)-tetrahydrofuran-2-ylmethyl]amino)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(2-methoxyethyl)carbamoyl][(2S)-tetrahydrofuran-2-ylmethyl]amino}-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-({[2-(propan-2-yloxy)ethyl]carbamoyl}[(2S)-tetrahydrofuran-2-ylmethyl]amino)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-[5-(4-chlorophenyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;-   4-[(1-butanoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(3-methoxy-2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropanoyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(cyclohexylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2R)-2-hydroxybutyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[(1-methyl-1H-pyrazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethyl-1H-pyrazol-4-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-{[3-(1-methyl-1H-pyrrol-2-yl)propanoyl](tetrahydrofuran-2-ylmethyl)amino}-1,3-thiazole-5-carboxamide;-   2-{[(1,5-dimethyl-1H-pyrazol-3-yl)acetyl](tetrahydrofuran-2-ylmethyl)amino}-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(tetrahydrofuran-2-ylmethyl)(1,3-thiazol-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-[(4-cyanobenzyl)(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-6-yl)methyl]-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3-methylbutanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   5-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-{1-[(1-methylpiperidin-4-yl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(propan-2-ylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   5-[1-(phenylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide;-   4-(phenylsulfonyl)-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(phenylsulfonyl)benzamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIIB)

In another aspect, the present invention provides compounds of Formula(VIIIB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (VIIIB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

In one embodiment of Formula (VIIIB), X is N or CY¹. In anotherembodiment of Formula (VIIIB), X is N. In another embodiment of Formula(VIIIB), X is CY¹.

In one embodiment of Formula (VIIIB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (VIIIB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (VIIIB), X is CY¹; and Y¹ is Cl. In another embodiment ofFormula (VIIIB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (VIIIB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (VIIIB), R³ is independently selected from the group consistingof phenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (VIIIB), R³ is phenyl; wherein each R³phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SO₂R⁴,C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; andwherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of F, Cl,Br and I. In another embodiment of Formula (VIIIB), R³ is 5-6 memberedheteroaryl; wherein each R³ 5-6 membered heteroaryl is substituted withone, two, three or four substituents independently selected from thegroup consisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(VIIIB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (VIIIB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (VIIIB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (VIIIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIIB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIIB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (VIIIB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (VIIIB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (VIIIB), R⁷, at each occurrence, isalkyl or heterocyclyl.

In one embodiment of Formula (VIIIB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (VIIIB), R⁸, at eachoccurrence, is independently alkyl.

In one embodiment of Formula (VIIIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (VIIIB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (VIIIB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(VIIIB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (VIIIB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂CHCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH. In another embodiment of Formula (VIIIB), R¹¹,at each occurrence, is independently alkyl. In another embodiment ofFormula (VIIIB), R¹¹, at each occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (VIIIB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R¹¹, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the proviso that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent.

Still another embodiment pertains to compounds having Formula (VIIIB),which include

-   tert-butyl    4-[4-(imidazo[1,2-a]pyridin-7-ylcarbamoyl)phenyl]piperidine-1-carboxylate;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IXB)

In another aspect, the present invention provides compounds of Formula(IXB)

and pharmaceutically acceptable salts thereof; wherein X and R³ are asdescribed herein for Formula (I).

One embodiment pertains to compounds of Formula (IXB) orpharmaceutically acceptable salts thereof;

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen,alkyl, alkoxy, haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴,OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴,NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴,NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴,C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R³ phenyl is optionally additionally substitutedwith one substituent independently selected from the group consisting ofalkyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent; and

when X is CY¹ and Y¹ is hydrogen; and R³ is phenyl; the R³ phenyl is notsubstituted at the para position with phenyl.

In one embodiment of Formula (IXB), X is N or CY¹. In another embodimentof Formula (IXB), X is N. In another embodiment of Formula (IXB), X isCY¹.

In one embodiment of Formula (IXB), X is CY¹; and Y¹ is independentlyselected from the group consisting of hydrogen, alkyl, alkoxy,haloalkyl, hydroxyalkyl, OH, CN, F, Cl, Br, and I. In another embodimentof Formula (IXB), X is CY¹; and Y¹ is independently selected from thegroup consisting of hydrogen, Cl, Br, and I. In another embodiment ofFormula (IXB), X is CY¹; and Y¹ is Cl. In another embodiment of Formula(IXB), X is CY¹; and Y¹ is hydrogen.

In one embodiment of Formula (IXB), R³ is independently selected fromthe group consisting of phenyl and 5-6 membered heteroaryl; wherein eachR³ phenyl is substituted at the para position with one substituentindependently selected from the group consisting of R⁴, OR⁴, SR⁴,S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂,NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴,NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂,C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴,C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁴, C(N)N(R⁴)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R³ phenyl is optionally additionally substituted with onesubstituent independently selected from the group consisting of alkyl,haloalkyl, alkoxyalkyl, hydroxyalkyl, C(O)H, C(O)OH, C(N)NH₂, OH, CN,N₃, NO₂, F, Cl, Br and I; wherein each R³ 5-6 membered heteroaryl issubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴,C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂,NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴,C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂,SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁴, C(N)N(R⁴)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. In another embodiment ofFormula (IXB), R³ is independently selected from the group consisting ofphenyl and 5-6 membered heteroaryl; wherein each R³ phenyl issubstituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)NHR⁴, C(O)NHR⁴, F,Cl, Br and I.

In one embodiment of Formula (IXB), R³ is phenyl; wherein each R³ phenylis substituted at the para position with one substituent independentlyselected from the group consisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴,NR⁴C(O)R⁴, NHS(O)₂R⁴, NHC(O)OR⁴, and C(O)NHR⁴; and wherein each R³phenyl is optionally additionally substituted with one substituentindependently selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IXB), R³ is 5-6 membered heteroaryl;wherein each R³ 5-6 membered heteroaryl is substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I. In another embodiment of Formula(IXB), R³ is thienyl; wherein each R³ thienyl is substituted with one,two, or three substituents independently selected from the groupconsisting of R⁴, C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴,NR⁴C(O)NHR⁴, C(O)NHR⁴, F, Cl, Br and I.

In one embodiment of Formula (IXB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (IXB), R⁴, at each occurrence,is independently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (IXB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IXB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (IXB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (IXB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (IXB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IXB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (IXB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (IXB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (IXB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IXB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (IXB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(IXB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (IXB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

In another embodiment of Formula (IXB), R¹, at each occurrence, isindependently alkyl. In another embodiment of Formula (IXB), R¹¹, ateach occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (IXB)

wherein

X is N or CY¹;

Y¹ is independently selected from the group consisting of hydrogen, F,Cl, Br, and I;

R³ is independently selected from the group consisting of phenyl and 5-6membered heteroaryl; wherein each R³ phenyl is substituted at the paraposition with one substituent independently selected from the groupconsisting of R⁴, OR⁴, SO₂R⁴, C(O)R⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴,NHC(O)OR⁴, C(O)NHR⁴, F, Cl, Br and I; wherein each R³ phenyl isoptionally additionally substituted with one substituent independentlyselected from the group consisting of F, Cl, Br and I; wherein each R³5-6 membered heteroaryl is substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁴,C(O)R⁴, NHR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, C(O)NHR⁴, F,Cl, Br and I;

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶, aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH;

with the provisos that

when X is CY¹ and Y¹ is hydrogen; and R³ is thiazolyl; the R³ thiazolylis substituted with one substituent; and when X is CY¹ and Y¹ ishydrogen; and R³ is phenyl; the R³ phenyl is not substituted at the paraposition with phenyl.

Still another embodiment pertains to compounds having Formula (IXB),which include

-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide;-   2-cyclopentyl-N-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}acetamide;-   tert-butyl    4-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}-3,6-dihydropyridine-1    (2H)-carboxylate;-   tert-butyl    4-[4-(imidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl]piperidine-1-carboxylate;-   tert-butyl    4-{4-[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]phenyl}piperidine-1-carboxylate;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (XB)

In another aspect, the present invention provides compounds of Formula(XB)

and pharmaceutically acceptable salts thereof; wherein R⁴ is asdescribed herein for Formula (IB).

One embodiment pertains to compounds of Formula (XB) or pharmaceuticallyacceptable salts thereof;

wherein

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl,and 3-12 membered heterocyclyl; wherein each R⁴ alkyl, alkenyl, andalkynyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁵,OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵,N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵,NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵,NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵,C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12 memberedheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁶,OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, OC(O)R⁶, OC(O)OR⁶,NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶,NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁷, OR⁷, SR⁷,S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂,NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷,NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂,C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷,C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, N₃, NO₂, F, Cl, Br and I; wherein each R⁷ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, and alkynyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl,and cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of aryl, alkoxy, OH,CN, NO₂, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl,cycloalkenyl, and heterocyclyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, NH₂, NHR¹¹,N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H,C(O)OH, COH, CN, NO₂, F, Cl, Br and I; and

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹⁰ alkyl, alkenyl, and alkynyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of alkoxy, F, Cl, Brand I; and

R¹¹, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl,alkenyl, and alkynyl; wherein each R¹¹ alkyl is optionally substitutedwith NH(CH₃), heterocyclyl, SCH₂CH(NH₂)C(O)OH,OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂CHCH₂CH₂NH₂, or NHC(O)CH₂CH(NH₂)C(O)OH.

In one embodiment of Formula (XB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, cycloalkyl, cycloalkenyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵,OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵,NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂,NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH,C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁵, C(N)N(R⁵)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein each R⁴ aryl, cycloalkyl, cycloalkenyl, and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂,NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶,NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶,NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶,C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁶, C(N)N(R⁶)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I. In another embodiment of Formula (XB), R⁴, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,cycloalkyl, and 3-12 membered heterocyclyl; wherein each R⁴ alkyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁵, OR⁵, C(O)R⁵,NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl, cycloalkyl and 3-12membered heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶, NHC(O)R⁶, C(O)N(R⁶)₂, OH,and F.

In another embodiment of Formula (XB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷,OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R, NR⁷S(O)₂R⁷,NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁵ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, SR⁸,S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂,NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸,NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂,C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸,C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (XB), R⁵, at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁵ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁷, OR⁷, and OH; wherein each R⁵aryl and heterocyclyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁸, OR⁸, CN, F, Cl, Br and I.

In one embodiment of Formula (XB), R⁶, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹,OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹,NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹,NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹,C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclylis optionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰,S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰,N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰,NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰,NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰,C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂,F, Cl, Br and I. In another embodiment of Formula (XB), R⁶, at eachoccurrence, is independently selected from the group consisting ofalkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl;wherein each R⁶ alkyl and alkenyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH, F, Cl, Br and I; whereineach R⁶ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, CN, F, Cl, Br and I.

In one embodiment of Formula (XB), R⁷, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, N₃, NO₂, F, Cl, Br and I; whereineach R⁷ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (XB), R⁷, at each occurrence, is alkylor heterocyclyl.

In one embodiment of Formula (XB), R⁸, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl, andalkynyl. In another embodiment of Formula (XB), R⁸, at each occurrence,is independently alkyl.

In one embodiment of Formula (XB), R⁹, at each occurrence, isindependently selected from the group consisting of alkyl, alkenyl,alkynyl, aryl, heterocyclyl, cycloalkyl, and cycloalkenyl; wherein eachR⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of aryl, alkoxy, OH, CN, NO₂, F, Cl, Br and I; wherein eachR⁹ aryl, cycloalkyl, cycloalkenyl, and heterocyclyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹,OC(O)R¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, C(O)NH₂,C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)H, C(O)OH, COH, CN, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (XB), R⁹ at each occurrence, isindependently selected from the group consisting of alkyl, aryl,heterocyclyl, and cycloalkyl; wherein each R⁹ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of aryl, and alkoxy; wherein each R⁹aryl, cycloalkyl, and heterocyclyl is optionally substituted with one,two, three or four substituents independently selected from the groupconsisting of R¹¹, OR¹¹, C(O)R¹¹, CO(O)R¹¹, and F.

In one embodiment of Formula (XB), R¹⁰, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹⁰alkyl, alkenyl, and alkynyl is optionally substituted with one, two,three or four substituents independently selected from the groupconsisting of alkoxy, F, Cl, Br and I. In another embodiment of Formula(XB), R¹⁰, at each occurrence, is independently heterocyclyl,cycloalkyl, alkyl, or alkenyl; wherein each R¹⁰ alkyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of alkoxy, and F.

In one embodiment of Formula (XB), R¹¹, at each occurrence, isindependently selected from the group consisting of aryl, heterocyclyl,cycloalkyl, cycloalkenyl, alkyl, alkenyl, and alkynyl; wherein each R¹¹alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH. In another embodiment of Formula (XB), R¹, ateach occurrence, is independently alkyl. In another embodiment ofFormula (XB), R¹, at each occurrence, is independently cycloalkyl.

One embodiment pertains to compounds or pharmaceutically acceptablesalts thereof, which are useful as inhibitors of NAMPT, the compoundshaving Formula (XB)

wherein

R⁴, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, cycloalkyl, and 3-12 membered heterocyclyl;wherein each R⁴ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofR⁵, OR⁵, C(O)R⁵, NHC(O)R⁵, OH, F, Cl, Br and I; wherein each R⁴ aryl,cycloalkyl, and 3-12 membered heterocyclyl is optionally substitutedwith one, two, three or four substituents independently selected fromthe group consisting of R⁶, OR⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, C(O)C(O)R⁶,NHC(O)R⁶, NHC(O)NHR⁶, C(O)N(R⁶)₂, OH, F, Cl, Br and I;

R⁵, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁵alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R⁷,OR⁷, OH, F, Cl, Br and I; wherein each R⁵ aryl, and heterocyclyl isoptionally substituted with one, two, three or four substituentsindependently selected from the group consisting of R⁸, OR⁸, CN, F, Cl,Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of alkyl, alkenyl, aryl, heterocyclyl, cycloalkyl, andcycloalkenyl; wherein each R⁶ alkyl and alkenyl is optionallysubstituted with one, two, three or four substituents independentlyselected from the group consisting of R⁹, OR⁹, SO₂R⁹, NH₂, N(R⁹)₂, OH,F, Cl, Br and I; wherein each R⁶ aryl, cycloalkyl, cycloalkenyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹⁰,OR¹⁰, C(O)R¹⁰, CN, F, and Cl;

R⁷, at each occurrence, is independently selected from the groupconsisting of alkyl, and heterocyclyl;

R⁸, at each occurrence, is independently alkyl;

R⁹, at each occurrence, is independently selected from the groupconsisting of alkyl, aryl, heterocyclyl, and cycloalkyl; wherein each R⁹alkyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of aryl,alkoxy, F, Cl, Br and I; wherein each R⁹ aryl, cycloalkyl, andheterocyclyl is optionally substituted with one, two, three or foursubstituents independently selected from the group consisting of R¹¹,OR¹¹, C(O)R¹¹, CO(O)R, CN, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of aryl, heterocyclyl, cycloalkyl, alkyl, and alkenyl;wherein each R¹⁰ alkyl is optionally substituted with one, two, three orfour substituents independently selected from the group consisting ofalkoxy, and F; and

R¹¹, at each occurrence, is independently cycloalkyl or alkyl; whereineach R¹¹ alkyl is optionally substituted with NH(CH₃), heterocyclyl,SCH₂CH(NH₂)C(O)OH, OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂OCH₂CH₂NH₂, orNHC(O)CH₂CH(NH₂)C(O)OH.

Still another embodiment pertains to compounds having Formula (XB),which include

-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   4-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-phenylthiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(methylsulfonyl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}pyrrolidine-1-carboxylate;-   5-{1-[(2R)-2-hydroxypropyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[(cyclopentylacetyl)amino]-3-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}benzamide;-   4-[1-(cyclopropylacetyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide;-   5-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(propan-2-yloxy)phenyl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(2-methylpropanoyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   5-[3-(benzoylamino)oxetan-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(tetrahydrofuran-3-ylacetyl)amino]oxetan-3-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(pentanoylamino)oxetan-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3R)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}benzamide;-   5-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-3-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-4-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(3-methoxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-butanoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3S)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{[(3S)-1-(3-hydroxy-3-methylbutanoyl)pyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   2-(4-benzoylpiperazin-1-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(propan-2-yl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-phenyl-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide;-   tert-butyl    4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2-yloxy)acetyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(1,4-dioxan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-(4-hydroxytetrahydro-2H-pyran-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}azetidine-1-carboxylate;-   tert-butyl    4-hydroxy-4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   5-{3-hydroxy-1-[(2S)-2-methylbutanoyl]azetidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[3-hydroxy-1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(3-{[(2S)-2-methylbutanoyl]amino}oxetan-3-yl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1-[1-(3-methylbutanoyl)piperidin-4-yl]-1H-pyrazole-3-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-[(1-acetylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylpiperidin-4-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(propan-2-yloxy)acetyl]piperidin-4-yl}oxy)benzamide;-   4-{[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]oxy}benzamide;-   4-{[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}benzamide;-   tert-butyl    (3R)-3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}pyrrolidine-1-carboxylate;-   4-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(3,3-difluorocyclobutyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[6-(morpholin-4-yl)pyridin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methyltetrahydro-2H-pyran-2-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   tert-butyl    4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylbutanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-{[(2S)-2-methylbutanoyl]amino}cyclobutyl)thiophene-2-carboxamide;-   5-[1-(benzoylamino)cyclobutyl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3,3,3-trifluoropropanoyl)amino]cyclobutyl}thiophene-2-carboxamide;-   N-(1-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}cyclobutyl)tetrahydro-2H-pyran-4-carboxamide;-   tert-butyl    3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}azetidine-1-carboxylate;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-2-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-3-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]furan-2-carboxamide;-   5-[1-(cyclobutylmethyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide;-   5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide;-   4-[1-(furan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(piperidin-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-phenoxybenzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide;-   4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide;-   5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(2,2-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclohexylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide;-   4-(1-butanoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylpent-2-enoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyloxetan-3-yl)carbonyl]piperidin-4-yl}benzamide;-   4-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-{1-[(1-cyanocyclopropyl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopentylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-oxobutanoyl)piperidin-4-yl]benzamide;-   4-{1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]piperidin-4-yl}benzamide;-   4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)piperidin-4-yl]benzamide;-   4-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-propanoylpiperidin-4-yl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)piperidin-4-yl]benzamide;-   4-[1-(2,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide;-   5-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   2-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide;-   4-[(cyclopentylacetyl)amino]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2-methylbutanoyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopropylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-(1-benzoylazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2-ylcarbonyl)azetidin-3-yl]benzamide;-   5-[4-hydroxy-1-(3-methylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[4-hydroxy-1-(2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-[1-(3,3-dimethylbutanoyl)-4-hydroxypiperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   5-(1-benzoyl-4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)benzamide;-   4-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[(1-benzoylazetidin-3-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   tert-butyl    4-{4-[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-1-ylcarbonyl)benzamide;-   4-[1-(ethylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)azetidin-3-yl]benzamide;-   propan-2-yl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   2-methylpropyl    4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]piperidin-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide;-   N-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   5-[1-(2-cyano-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;-   4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3R)-tetrahydrofuran-3-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)pyrrolidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]pyrrolidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]pyrrolidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)pyrrolidin-3-yl]benzamide;-   4-[1-(ethylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(cyclopropylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)pyrrolidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclopentylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylpentanoyl)azetidin-3-yl]benzamide;-   4-[1-(cyclopentylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,2-dimethylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-5-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-4-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(2-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(furan-2-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,4-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-3-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylbenzoyl)azetidin-3-yl]benzamide;-   4-[1-(4-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,2-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,5-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(4-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbutanoyl)azetidin-3-yl]benzamide;-   4-[1-(3,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3-cyanobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4-methoxybenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(cyclohexylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(cyclohexylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2-ylcarbonyl)azetidin-3-yl]benzamide;-   4-[1-(furan-3-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methylcyclohexyl)carbonyl]azetidin-3-yl}benzamide;-   4-[1-(2,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbenzoyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2-yl)carbonyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]azetidin-3-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)pyrrolidin-3-yl]benzamide;-   5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide;-   4-[1-(cyclopropylsulfonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   5-{(1R)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{(1R)-3-methyl-1-[(tetrahydrofuran-3-ylacetyl)amino]butyl}thiophene-2-carboxamide;-   5-{(1S)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1-phenylpiperidin-4-yl)-1,3-thiazole-5-carboxamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(pyridin-2-yl)piperidin-4-yl]-1,3-thiazole-5-carboxamide;-   5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;-   4-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)piperidin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2-(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide;-   N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[6-(trifluoromethyl)pyrimidin-4-yl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide;    and pharmaceutically acceptable salts thereof.

Pharmaceutical Compositions, Combination Therapies, Methods ofTreatment, and Administration

Another embodiment comprises pharmaceutical compositions comprising acompound having Formula (I) and an excipient.

Still another embodiment comprises methods of treating cancer in amammal comprising administering thereto a therapeutically acceptableamount of a compound having Formula (I).

Still another embodiment pertains to compositions for treating diseasesduring which NAMPT is expressed, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I).

Still another embodiment pertains to methods of treating disease in apatient during which NAMPT is expressed, said methods comprisingadministering to the patient a therapeutically effective amount of acompound having Formula (I).

Still another embodiment pertains to compositions for treatinginflammatory and tissue repair disorders; particularly rheumatoidarthritis, inflammatory bowel disease, asthma and COPD (chronicobstructive pulmonary disease), osteoarthritis, osteoporosis andfibrotic diseases; dermatosis, including psoriasis, atopic dermatitisand ultra-violet induced skin damage; autoimmune diseases includingsystemic lupus erythematosis, multiple sclerosis, psoriatic arthritis,ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease,stroke, athersclerosis, restenosis, diabetes, glomerulonephritis,cancer, particularly wherein the cancer is selected from breast,prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas,leukemia, lymphoma or Hodgkin's disease, cachexia, inflammationassociated with infection and certain viral infections, includingAcquired Immune Deficiency Syndrome (AIDS), adult respiratory distresssyndrome, and ataxia telengiectasia, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I).

Still another embodiment pertains to methods of treating inflammatoryand tissue repair disorders; particularly rheumatoid arthritis,inflammatory bowel disease, asthma and COPD (chronic obstructivepulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases;dermatosis, including psoriasis, atopic dermatitis and ultra-violetinduced skin damage; autoimmune diseases including systemic lupuserythematosis, multiple sclerosis, psoriatic arthritis, ankylosingspondylitis, tissue and organ rejection, Alzheimer's disease, stroke,athersclerosis, restenosis, diabetes, glomerulonephritis, cancer,particularly wherein the cancer is selected from breast, prostate, lung,colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphomaor Hodgkin's disease, cachexia, inflammation associated with infectionand certain viral infections, including Acquired Immune DeficiencySyndrome (AIDS), adult respiratory distress syndrome, and ataxiatelengiectasia in a patient, said methods comprising administering tothe patient a therapeutically effective amount of a compound havingFormula (I).

Still another embodiment pertains to compositions for treating diseasesduring which NAMPT is expressed, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I) and a therapeutically effective amount of one additionaltherapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating disease in apatient during which NAMPT is expressed, said methods comprisingadministering to the patient a therapeutically effective amount of acompound having Formula (I) and a therapeutically effective amount ofone additional therapeutic agent or more than one additional therapeuticagent.

Still another embodiment pertains to compositions for treatinginflammatory and tissue repair disorders; particularly rheumatoidarthritis, inflammatory bowel disease, asthma and COPD (chronicobstructive pulmonary disease), osteoarthritis, osteoporosis andfibrotic diseases; dermatosis, including psoriasis, atopic dermatitisand ultra-violet induced skin damage; autoimmune diseases includingsystemic lupus erythematosis, multiple sclerosis, psoriatic arthritis,ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease,stroke, athersclerosis, restenosis, diabetes, glomerulonephritis,cancer, particularly wherein the cancer is selected from breast,prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas,leukemia, lymphoma or Hodgkin's disease, cachexia, inflammationassociated with infection and certain viral infections, includingAcquired Immune Deficiency Syndrome (AIDS), adult respiratory distresssyndrome, and ataxia telengiectasia, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I) and a therapeutically effective amount of one additionaltherapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating inflammatoryand tissue repair disorders; particularly rheumatoid arthritis,inflammatory bowel disease, asthma and COPD (chronic obstructivepulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases;dermatosis, including psoriasis, atopic dermatitis and ultra-violetinduced skin damage; autoimmune diseases including systemic lupuserythematosis, multiple sclerosis, psoriatic arthritis, ankylosingspondylitis, tissue and organ rejection, Alzheimer's disease, stroke,athersclerosis, restenosis, diabetes, glomerulonephritis, cancer,particularly wherein the cancer is selected from breast, prostate, lung,colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphomaor Hodgkin's disease, cachexia, inflammation associated with infectionand certain viral infections, including Acquired Immune DeficiencySyndrome (AIDS), adult respiratory distress syndrome, and ataxiatelengiectasia in a patient, said methods comprising administering tothe patient a therapeutically effective amount of the compound havingFormula (I) and a therapeutically effective amount of one additionaltherapeutic agent or more than one additional therapeutic agent.

Metabolites of compounds having Formula (I), produced by in vitro or invivo metabolic processes, may also have utility for treating diseasesassociated with NAMPT.

Certain precursor compounds which may be metabolized in vitro or in vivoto form compounds having Formula (I) may also have utility for treatingdiseases associated with NAMPT.

Compounds having Formula (I) may exist as acid addition salts, basicaddition salts or zwitterions. Salts of the compounds are preparedduring isolation or following purification of the compounds. Acidaddition salts of the compounds are those derived from the reaction ofthe compounds with an acid. For example, the acetate, adipate, alginate,bicarbonate, citrate, aspartate, benzoate, benzenesulfonate, bisulfate,butyrate, camphorate, camphorsufonate, digluconate, formate, fumarate,glycerophosphate, glutamate, hemisulfate, heptanoate, hexanoate,hydrochloride, hydrobromide, hydroiodide, lactobionate, lactate,maleate, mesitylenesulfonate, methanesulfonate, naphthylenesulfonate,nicotinate, oxalate, pamoate, pectinate, persulfate, phosphate, picrate,propionate, succinate, tartrate, thiocyanate, trichloroacetic,trifluoroacetic, para-toluenesulfonate, and undecanoate salts of thecompounds are contemplated as being embraced by this invention. Basicaddition salts of the compounds are those derived from the reaction ofthe compounds with the hydroxide, carbonate or bicarbonate of cationssuch as lithium, sodium, potassium, calcium, and magnesium.

The compounds having Formula (I) may be administered, for example,bucally, ophthalmically, orally, osmotically, parenterally(intramuscularly, intraperitoneally intrasternally, intravenously,subcutaneously), rectally, topically, transdermally or vaginally.

Therapeutically effective amounts of compounds having Formula (I) dependon the recipient of the treatment, the disorder being treated and theseverity thereof, the composition containing the compound, the time ofadministration, the route of administration, the duration of treatment,the compound potency, its rate of clearance and whether or not anotherdrug is co-administered. The amount of a compound of this inventionhaving Formula (I) used to make a composition to be administered dailyto a patient in a single dose or in divided doses is from about 0.03 toabout 200 mg/kg body weight. Single dose compositions contain theseamounts or a combination of submultiples thereof.

Compounds having Formula (I) may be administered with or without anexcipient. Excipients include, for example, encapsulating materials oradditives such as absorption accelerators, antioxidants, binders,buffers, coating agents, coloring agents, diluents, disintegratingagents, emulsifiers, extenders, fillers, flavoring agents, humectants,lubricants, perfumes, preservatives, propellants, releasing agents,sterilizing agents, sweeteners, solubilizers, wetting agents andmixtures thereof.

Excipients for preparation of compositions comprising a compound havingFormula (I) to be administered orally in solid dosage form include, forexample, agar, alginic acid, aluminum hydroxide, benzyl alcohol, benzylbenzoate, 1,3-butylene glycol, carbomers, castor oil, cellulose,cellulose acetate, cocoa butter, corn starch, corn oil, cottonseed oil,cross-povidone, diglycerides, ethanol, ethyl cellulose, ethyl laureate,ethyl oleate, fatty acid esters, gelatin, germ oil, glucose, glycerol,groundnut oil, hydroxypropylmethyl cellulose, isopropanol, isotonicsaline, lactose, magnesium hydroxide, magnesium stearate, malt,mannitol, monoglycerides, olive oil, peanut oil, potassium phosphatesalts, potato starch, povidone, propylene glycol, Ringer's solution,safflower oil, sesame oil, sodium carboxymethyl cellulose, sodiumphosphate salts, sodium lauryl sulfate, sodium sorbitol, soybean oil,stearic acids, stearyl fumarate, sucrose, surfactants, talc, tragacanth,tetrahydrofurfuryl alcohol, triglycerides, water, and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered ophthalmically or orallyin liquid dosage forms include, for example, 1,3-butylene glycol, castoroil, corn oil, cottonseed oil, ethanol, fatty acid esters of sorbitan,germ oil, groundnut oil, glycerol, isopropanol, olive oil, polyethyleneglycols, propylene glycol, sesame oil, water and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered osmotically include, forexample, chlorofluorohydrocarbons, ethanol, water and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered parenterally include,for example, 1,3-butanediol, castor oil, corn oil, cottonseed oil,dextrose, germ oil, groundnut oil, liposomes, oleic acid, olive oil,peanut oil, Ringer's solution, safflower oil, sesame oil, soybean oil,U.S.P. or isotonic sodium chloride solution, water and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered rectally or vaginallyinclude, for example, cocoa butter, polyethylene glycol, wax andmixtures thereof.

Compounds having Formula (I) are expected to be useful when used withalkylating agents, angiogenesis inhibitors, antibodies, antimetabolites,antimitotics, antiproliferatives, antivirals, aurora kinase inhibitors,apoptosis promoters (for example, Bcl-xL, Bcl-w and Bfl-1) inhibitors,activators of death receptor pathway, Bcr-Abl kinase inhibitors, BiTE(Bi-Specific T cell Engager) antibodies, antibody drug conjugates,biologic response modifiers, cyclin-dependent kinase inhibitors, cellcycle inhibitors, cyclooxygenase-2 inhibitors, DVDs, leukemia viraloncogene homolog (ErbB2) receptor inhibitors, growth factor inhibitors,heat shock protein (HSP)-90 inhibitors, histone deacetylase (HDAC)inhibitors, hormonal therapies, immunologicals, inhibitors of inhibitorsof apoptosis proteins (IAPs), intercalating antibiotics, kinaseinhibitors, kinesin inhibitors, Jak2 inhibitors, mammalian target ofrapamycin inhibitors, microRNA's, mitogen-activated extracellularsignal-regulated kinase inhibitors, multivalent binding proteins,non-steroidal anti-inflammatory drugs (NSAIDs), poly ADP (adenosinediphosphate)-ribose polymerase (PARP) inhibitors, platinumchemotherapeutics, polo-like kinase (Plk) inhibitors, phosphoinositide-3kinase (PI3K) inhibitors, proteosome inhibitors, purine analogs,pyrimidine analogs, receptor tyrosine kinase inhibitors,retinoids/deltoids plant alkaloids, small inhibitory ribonucleic acids(siRNAs), topoisomerase inhibitors, ubiquitin ligase inhibitors, and thelike, and in combination with one or more of these agents.

BiTE antibodies are bi-specific antibodies that direct T-cells to attackcancer cells by simultaneously binding the two cells. The T-cell thenattacks the target cancer cell. Examples of BiTE antibodies includeadecatumumab (Micromet MT201), blinatumomab (Micromet MT103) and thelike. Without being limited by theory, one of the mechanisms by whichT-cells elicit apoptosis of the target cancer cell is by exocytosis ofcytolytic granule components, which include perforin and granzyme B.

SiRNAs are molecules having endogenous RNA bases or chemically modifiednucleotides. The modifications do not abolish cellular activity, butrather impart increased stability and/or increased cellular potency.Examples of chemical modifications include phosphorothioate groups,2′-deoxynucleotide, 2′-OCH₃-containing ribonucleotides,2′-F-ribonucleotides, 2′-methoxyethyl ribonucleotides, combinationsthereof and the like. The siRNA can have varying lengths (e.g., 10-200bps) and structures (e.g., hairpins, single/double strands, bulges,nicks/gaps, mismatches) and are processed in cells to provide activegene silencing. A double-stranded siRNA (dsRNA) can have the same numberof nucleotides on each strand (blunt ends) or asymmetric ends(overhangs). The overhang of 1-2 nucleotides can be present on the senseand/or the antisense strand, as well as present on the 5′- and/or the3′-ends of a given strand.

Multivalent binding proteins are binding proteins comprising two or moreantigen binding sites. Multivalent binding proteins are engineered tohave the three or more antigen binding sites and are generally notnaturally occurring antibodies. The term “multispecific binding protein”means a binding protein capable of binding two or more related orunrelated targets. Dual variable domain (DVD) binding proteins aretetravalent or multivalent binding proteins binding proteins comprisingtwo or more antigen binding sites. Such DVDs may be monospecific (i.e.,capable of binding one antigen) or multispecific (i.e., capable ofbinding two or more antigens). DVD binding proteins comprising two heavychain DVD polypeptides and two light chain DVD polypeptides are referredto as DVD Ig's. Each half of a DVD Ig comprises a heavy chain DVDpolypeptide, a light chain DVD polypeptide, and two antigen bindingsites. Each binding site comprises a heavy chain variable domain and alight chain variable domain with a total of 6 CDRs involved in antigenbinding per antigen binding site.

Alkylating agents include altretamine, AMD-473, AP-5280, apaziquone,bendamustine, brostallicin, busulfan, carboquone, carmustine (BCNU),chlorambucil, CLORETAZINE® (laromustine, VNP 40101M), cyclophosphamide,decarbazine, estramustine, fotemustine, glufosfamide, ifosfamide,KW-2170, lomustine (CCNU), mafosfamide, melphalan, mitobronitol,mitolactol, nimustine, nitrogen mustard N-oxide, ranimustine,temozolomide, thiotepa, TREANDA® (bendamustine), treosulfan,trofosfamide and the like.

Angiogenesis inhibitors include endothelial-specific receptor tyrosinekinase (Tie-2) inhibitors, epidermal growth factor receptor (EGFR)inhibitors, insulin growth factor-2 receptor (IGFR-2) inhibitors, matrixmetalloproteinase-2 (MMP-2) inhibitors, matrix metalloproteinase-9(MMP-9) inhibitors, platelet-derived growth factor receptor (PDGFR)inhibitors, thrombospondin analogs, vascular endothelial growth factorreceptor tyrosine kinase (VEGFR) inhibitors and the like.

Antimetabolites include ALIMTA® (pemetrexed disodium, LY231514, MTA),5-azacitidine, XELODA® (capecitabine), carmofur, LEUSTAT® (cladribine),clofarabine, cytarabine, cytarabine ocfosfate, cytosine arabinoside,decitabine, deferoxamine, doxifluridine, eflornithine, EICAR(5-ethynyl-1-β-D-ribofuranosylimidazole-4-carboxamide), enocitabine,ethnylcytidine, fludarabine, 5-fluorouracil alone or in combination withleucovorin, GEMZAR® (gemcitabine), hydroxyurea, ALKERAN®(melphalan),mercaptopurine, 6-mercaptopurine riboside, methotrexate, mycophenolicacid, nelarabine, nolatrexed, ocfosfate, pelitrexol, pentostatin,raltitrexed, Ribavirin, triapine, trimetrexate, S-1, tiazofurin,tegafur, TS-1, vidarabine, UFT and the like.

Antivirals include ritonavir, hydroxychloroquine and the like.

Aurora kinase inhibitors include ABT-348, AZD-1152, MLN-8054, VX-680,Aurora A-specific kinase inhibitors, Aurora B-specific kinase inhibitorsand pan-Aurora kinase inhibitors and the like.

Bcl-2 protein inhibitors include AT-101 ((−)gossypol), GENASENSE® (G3139or oblimersen (Bcl-2-targeting antisense oligonucleotide)), IPI-194,IPI-565,N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-nitrobenzenesulfonamide)(ABT-737),N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide(ABT-263), GX-070 (obatoclax) and the like.

Bcr-Abl kinase inhibitors include DASATINIB® (BMS-354825), GLEEVEC®(imatinib) and the like.

CDK inhibitors include AZD-5438, BMI-1040, BMS-032, BMS-387, CVT-2584,flavopyridol, GPC-286199, MCS-5A, PD0332991, PHA-690509, seliciclib(CYC-202, R-roscovitine), ZK-304709 and the like.

COX-2 inhibitors include ABT-963, ARCOXIA® (etoricoxib), BEXTRA®(valdecoxib), BMS347070, CELEBREX® (celecoxib), COX-189 (lumiracoxib),CT-3, DERAMAXX® (deracoxib), JTE-522,4-methyl-2-(3,4-dimethylphenyl)-1-(4-sulfamoylphenyl-1H-pyrrole), MK-663(etoricoxib), NS-398, parecoxib, RS-57067, SC-58125, SD-8381, SVT-2016,S-2474, T-614, VIOXX® (rofecoxib) and the like.

EGFR inhibitors include ABX-EGF, anti-EGFR immunoliposomes, EGF-vaccine,EMD-7200, ERBITUX® (cetuximab), HR³, IgA antibodies, IRESSA®(gefitinib), TARCEVA® (erlotinib or OSI-774), TP-38, EGFR fusionprotein, TYKERB® (lapatinib) and the like.

ErbB2 receptor inhibitors include CP-724-714, CI-1033 (canertinib),HERCEPTIN® (trastuzumab), TYKERB® (lapatinib), OMNITARG® (2C4,petuzumab), TAK-165, GW-572016 (ionafarnib), GW-282974, EKB-569, PI-166,dHER2 (HER2 vaccine), APC-8024 (HER-2 vaccine), anti-HER/2neu bispecificantibody, B7.her2IgG3, AS HER2 trifunctional bispecfic antibodies, mABAR-209, mAB 2B-1 and the like.

Histone deacetylase inhibitors include depsipeptide, LAQ-824, MS-275,trapoxin, suberoylanilide hydroxamic acid (SAHA), TSA, valproic acid andthe like.

HSP-90 inhibitors include 17-AAG-nab, 17-AAG, CNF-101, CNF-1010,CNF-2024, 17-DMAG, geldanamycin, IPI-504, KOS-953, MYCOGRAB® (humanrecombinant antibody to HSP-90), NCS-683664, PU24FC1, PU-3, radicicol,SNX-2112, STA-9090 VER49009 and the like.

Inhibitors of inhibitors of apoptosis proteins include HGS1029,GDC-0145, GDC-0152, LCL-161, LBW-242 and the like.

Antibody drug conjugates include anti-CD22-MC-MMAF, anti-CD22-MC-MMAE,anti-CD22-MCC-DM1, CR-011-vcMMAE, PSMA-ADC, MEDI-547, SGN-19Am SGN-35,SGN-75 and the like

Activators of death receptor pathway include TRAIL, antibodies or otheragents that target TRAIL or death receptors (e.g., DR4 and DR5) such asApomab, conatumumab, ETR2-ST01, GDC0145 (lexatumumab), HGS-1029,LBY-135, PRO-1762 and trastuzumab.

Kinesin inhibitors include Eg5 inhibitors such as AZD4877, ARRY-520;CENPE inhibitors such as GSK923295A and the like.

JAK-2 inhibitors include CEP-701 (lesaurtinib), XL019 and INCB018424 andthe like.

MEK inhibitors include ARRY-142886, ARRY-438162 PD-325901, PD-98059 andthe like.

mTOR inhibitors include AP-23573, CCI-779, everolimus, RAD-001,rapamycin, temsirolimus, ATP-competitive TORC1/TORC2 inhibitors,including PI-103, PP242, PP30, Torin 1 and the like.

Non-steroidal anti-inflammatory drugs include AMIGESIC® (salsalate),DOLOBID® (diflunisal), MOTRIN® (ibuprofen), ORUDIS® (ketoprofen),RELAFEN® (nabumetone), FELDENE® (piroxicam), ibuprofen cream, ALEVE®(naproxen) and NAPROSYN® (naproxen), VOLTAREN® (diclofenac), INDOCIN®(indomethacin), CLINORIL® (sulindac), TOLECTIN® (tolmetin), LODINE®(etodolac), TORADOL® (ketorolac), DAYPRO® (oxaprozin) and the like.

PDGFR inhibitors include C-451, CP-673, CP-868596 and the like.

Platinum chemotherapeutics include cisplatin, ELOXATIN® (oxaliplatin)eptaplatin, lobaplatin, nedaplatin, PARAPLATIN® (carboplatin),satraplatin, picoplatin and the like.

Polo-like kinase inhibitors include BI-2536 and the like.

Phosphoinositide-3 kinase (PI3K) inhibitors include wortmannin,LY294002, XL-147, CAL-120, ONC-21, AEZS-127, ETP-45658, PX-866,GDC-0941, BGT226, BEZ235, XL765 and the like.

Thrombospondin analogs include ABT-510, ABT-567, ABT-898, TSP-1 and thelike.

VEGFR inhibitors include AVASTIN® (bevacizumab), ABT-869, AEE-788,ANGIOZYME™ (a ribozyme that inhibits angiogenesis (RibozymePharmaceuticals (Boulder, Colo.) and Chiron, (Emeryville, Calif.)),axitinib (AG-13736), AZD-2171, CP-547,632, IM-862, MACUGEN (pegaptamib),NEXAVAR® (sorafenib, BAY43-9006), pazopanib (GW-786034), vatalanib(PTK-787, ZK-222584), SUTENT® (sunitinib, SU-11248), VEGF trap, ZACTIMA™(vandetanib, ZD-6474) and the like.

Antibiotics include intercalating antibiotics aclarubicin, actinomycinD, amrubicin, annamycin, adriamycin, BLENOXANE® (bleomycin),daunorubicin, CAELYX® or MYOCET® (liposomal doxorubicin), elsamitrucin,epirbucin, glarbuicin, ZAVEDOS® (idarubicin), mitomycin C, nemorubicin,neocarzinostatin, peplomycin, pirarubicin, rebeccamycin, stimalamer,streptozocin, VALSTAR® (valrubicin), zinostatin and the like.

Topoisomerase inhibitors include aclarubicin, 9-aminocamptothecin,amonafide, amsacrine, becatecarin, belotecan, BN-80915, CAMPTOSAR®(irinotecan hydrochloride), camptothecin, CARDIOXANE® (dexrazoxine),diflomotecan, edotecarin, ELLENCE® or PHARMORUBICIN® (epirubicin),etoposide, exatecan, 10-hydroxycamptothecin, gimatecan, lurtotecan,mitoxantrone, orathecin, pirarbucin, pixantrone, rubitecan, sobuzoxane,SN-38, tafluposide, topotecan and the like.

Antibodies include AVASTIN® (bevacizumab), CD40-specific antibodies,chTNT-1/B, denosumab, ERBITUX® (cetuximab), HUMAX-CD4® (zanolimumab),IGF1R-specific antibodies, lintuzumab, PANOREX® (edrecolomab), RENCAREX®(WX G250), RITUXAN® (rituximab), ticilimumab, trastuzimab, CD20antibodies types I and II and the like.

Hormonal therapies include ARIMIDEX® (anastrozole), AROMASIN®(exemestane), arzoxifene, CASODEX® (bicalutamide), CETROTIDE®(cetrorelix), degarelix, deslorelin, DESOPAN® (trilostane),dexamethasone, DROGENIL® (flutamide), EVISTA® (raloxifene), AFEMA™(fadrozole), FARESTON® (toremifene), FASLODEX® (fulvestrant), FEMARA®(letrozole), formestane, glucocorticoids, HECTOROL® (doxercalciferol),RENAGEL® (sevelamer carbonate), lasofoxifene, leuprolide acetate,MEGACE® (megesterol), MIFEPREX® (mifepristone), NILANDRON™ (nilutamide),NOLVADEX® (tamoxifen citrate), PLENAXIS™ (abarelix), prednisone,PROPECIA® (finasteride), rilostane, SUPREFACT® (buserelin), TRELSTAR®(luteinizing hormone releasing hormone (LHRH)), VANTAS® (Histrelinimplant), VETORYL® (trilostane or modrastane), ZOLADEX® (fosrelin,goserelin) and the like.

Deltoids and retinoids include seocalcitol (EB1089, CB1093),lexacalcitrol (KH1060), fenretinide, PANRETIN® (aliretinoin), ATRAGEN®(liposomal tretinoin), TARGRETIN® (bexarotene), LGD-1550 and the like.

PARP inhibitors include ABT-888 (veliparib), olaparib, KU-59436,AZD-2281, AG-014699, BSI-201, BGP-15, INO-1001, ONO-2231 and the like.

Plant alkaloids include, but are not limited to, vincristine,vinblastine, vindesine, vinorelbine and the like.

Proteasome inhibitors include VELCADE® (bortezomib), MG132, NPI-0052,PR-171 and the like.

Examples of immunologicals include interferons and otherimmune-enhancing agents. Interferons include interferon alpha,interferon alpha-2a, interferon alpha-2b, interferon beta, interferongamma-1a, ACTIMMUNE® (interferon gamma-1b) or interferon gamma-n1,combinations thereof and the like. Other agents include ALFAFERONE®,(IFN-α), BAM-002 (oxidized glutathione), BEROMUN® (tasonermin), BEXXAR®(tositumomab), CAMPATH® (alemtuzumab), CTLA4 (cytotoxic lymphocyteantigen 4), decarbazine, denileukin, epratuzumab, GRANOCYTE®(lenograstim), lentinan, leukocyte alpha interferon, imiquimod, MDX-010(anti-CTLA-4), melanoma vaccine, mitumomab, molgramostim, MYLOTARG™(gemtuzumab ozogamicin), NEUPOGEN® (filgrastim), OncoVAC-CL, OVAREX®(oregovomab), pemtumomab (Y-muHMFG1), PROVENGE® (sipuleucel-T),sargaramostim, sizofilan, teceleukin, THERACYS® (BacillusCalmette-Guerin), ubenimex, VIRULIZIN® (immunotherapeutic, LorusPharmaceuticals), Z-100 (Specific Substance of Maruyama (SSM)), WF-10(Tetrachlorodecaoxide (TCDO)), PROLEUKIN® (aldesleukin), ZADAXIN®(thymalfasin), ZENAPAX® (daclizumab), ZEVALIN® (90Y-Ibritumomabtiuxetan) and the like.

Biological response modifiers are agents that modify defense mechanismsof living organisms or biological responses, such as survival, growth ordifferentiation of tissue cells to direct them to have anti-tumoractivity and include krestin, lentinan, sizofiran, picibanil PF-3512676(CpG-8954), ubenimex and the like.

Pyrimidine analogs include cytarabine (ara C or Arabinoside C), cytosinearabinoside, doxifluridine, FLUDARA® (fludarabine), 5-FU(5-fluorouracil), floxuridine, GEMZAR® (gemcitabine), TOMUDEX®(ratitrexed), TROXATYL™ (triacetyluridine troxacitabine) and the like.

Purine analogs include LANVIS® (thioguanine) and PURI-NETHOL®(mercaptopurine).

Antimitotic agents include batabulin, epothilone D (KOS-862),N-(2-((4-hydroxyphenyl)amino)pyridin-3-yl)-4-methoxybenzenesulfonamide,ixabepilone (BMS 247550), paclitaxel, TAXOTERE® (docetaxel), PNU100940(109881), patupilone, XRP-9881 (larotaxel), vinflunine, ZK-EPO(synthetic epothilone) and the like.

Ubiquitin ligase inhibitors include MDM2 inhibitors, such as nutlins,NEDD8 inhibitors such as MLN4924 and the like.

Compounds of this invention can also be used as radiosensitizers thatenhance the efficacy of radiotherapy. Examples of radiotherapy includeexternal beam radiotherapy, teletherapy, brachytherapy and sealed,unsealed source radiotherapy and the like.

Additionally, compounds having Formula (I) may be combined with otherchemotherapeutic agents such as ABRAXANE™ (ABI-007), ABT-100 (farnesyltransferase inhibitor), ADVEXIN® (Ad5CMV-p53 vaccine), ALTOCOR® orMEVACOR® (lovastatin), AMPLIGEN® (poly I:poly C12U, a synthetic RNA),APTOSYN® (exisulind), AREDIA® (pamidronic acid), arglabin,L-asparaginase, atamestane (1-methyl-3,17-dione-androsta-1,4-diene),AVAGE® (tazarotene), AVE-8062 (combreastatin derivative) BEC2(mitumomab), cachectin or cachexin (tumor necrosis factor), canvaxin(vaccine), CEAVAC® (cancer vaccine), CELEUK® (celmoleukin), CEPLENE®(histamine dihydrochloride), CERVARIX® (human papillomavirus vaccine),CHOP® (C: CYTOXAN® (cyclophosphamide); H: ADRIAMYCIN®(hydroxydoxorubicin); O: Vincristine (ONCOVIN®); P: prednisone), CYPAT™(cyproterone acetate), combrestatin A4P, DAB(389)EGF (catalytic andtranslocation domains of diphtheria toxin fused via a His-Ala linker tohuman epidermal growth factor) or TransMID-107R™ (diphtheria toxins),dacarbazine, dactinomycin, 5,6-dimethylxanthenone-4-acetic acid (DMXAA),eniluracil, EVIZON™ (squalamine lactate), DIMERICINE® (T4N5 liposomelotion), discodermolide, DX-8951 f (exatecan mesylate), enzastaurin,EP0906 (epithilone B), GARDASIL® (quadrivalent human papillomavirus(Types 6, 11, 16, 18) recombinant vaccine), GASTRIMMUNE®, GENASENSE®,GMK (ganglioside conjugate vaccine), GVAX® (prostate cancer vaccine),halofuginone, histerelin, hydroxycarbamide, ibandronic acid, IGN-101,IL-13-PE38, IL-13-PE38QQR (cintredekin besudotox), IL-13-pseudomonasexotoxin, interferon-α, interferon-γ, JUNOVAN™ or MEPACT™ (mifamurtide),lonafarnib, 5,10-methylenetetrahydrofolate, miltefosine(hexadecylphosphocholine), NEOVASTAT®(AE-941), NEUTREXIN® (trimetrexateglucuronate), NIPENT® (pentostatin), ONCONASE® (a ribonuclease enzyme),ONCOPHAGE® (melanoma vaccine treatment), ONCOVAX® (IL-2 Vaccine),ORATHECIN™ (rubitecan), OSIDEM® (antibody-based cell drug), OVAREX® MAb(murine monoclonal antibody), paclitaxel, PANDIMEX™ (aglycone saponinsfrom ginseng comprising 20(S)protopanaxadiol (aPPD) and20(S)protopanaxatriol (aPPT)), panitumumab, PANVAC®-VF (investigationalcancer vaccine), pegaspargase, PEG Interferon A, phenoxodiol,procarbazine, rebimastat, REMOVAB® (catumaxomab), REVLIMID®(lenalidomide), RSR13 (efaproxiral), SOMATULINE® LA (lanreotide),SORIATANE® (acitretin), staurosporine (Streptomyces staurospores),talabostat (PT100), TARGRETIN® (bexarotene), TAXOPREXIN®(DHA-paclitaxel), TELCYTA® (canfosfamide, TLK286), temilifene, TEMODAR®(temozolomide), tesmilifene, thalidomide, THERATOPE® (STn-KLH), thymitaq(2-amino-3,4-dihydro-6-methyl-4-oxo-5-(4-pyridylthio)quinazolinedihydrochloride), TNFERADE™ (adenovector: DNA carrier containing thegene for tumor necrosis factor-a), TRACLEER® or ZAVESCA® (bosentan),tretinoin (Retin-A), tetrandrine, TRISENOX® (arsenic trioxide),VIRULIZIN®, ukrain (derivative of alkaloids from the greater celandineplant), vitaxin (anti-alphavbeta3 antibody), XCYTRIN® (motexafingadolinium), XINLAY™ (atrasentan), XYOTAX™ (paclitaxel poliglumex),YONDELIS® (trabectedin), ZD-6126, ZINECARD® (dexrazoxane), ZOMETA®(zolendronic acid), zorubicin and the like.

Data

Determination of the utility of compounds having Formula (I) as bindersto and inhibitors of NAMPT was performed using Time-ResolvedFluorescence Resonance Energy Transfer (TR-FRET) binding assays.

Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) BindingAssay of NAMPT

Test compounds were serially diluted (typically 11 half log dilutions)in neat DMSO to 50× final concentrations prior to dilution with assaybuffer (50 mM HEPES (NaOH), pH 7.5, 100 mM NaCl, 10 mM MgCl₂, 1 mM DTT,1% Glycerol) to 3× and 6% DMSO. Six μL were transferred to 384-welllow-volume plates (Owens Corning #3673). To this, 12 L of a 1.5×solution containing enzyme, probe and antibody were added. Finalconcentrations in the 18 μL reactions were 1× assay buffer, 2% DMSO, 6.8nM NAMPT (human, recombinant, C-terminally His-tagged), 200 nM probe (apotent nicotinamide-competitive inhibitor conjugated to Oregon Green488) and 1 nM Tb-anti-His antibody (Invitrogen #PV5895).

Reactions were equilibrated at room temperature for 3 hours prior toreading on an Envision multi-label plate reader (Perkin Elmer; Ex=337nm, Em=520 and 495 nm). Time-resolved FRET ratios (Em₅₂₀/Em₄₉₅) werenormalized to controls, plotted as a function of compound concentrationand fit with the four-parameter logistic equation to determine IC50s.

Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) BindingAssay of NAMPT with PRPP

Compound handling and data processing were identical to the assay in theabsence of substrates (above). Final concentrations were 1× assaybuffer, 2% DMSO, 2 nM NAMPT, 2 nM probe, 1 nM Tb-anti-His antibody(Invitrogen #PV5895), 200 M PRPP and 2.5 mM ATP. Reactions wereequilibrated for 16 hours prior to measurement to allow for potentialenzymatic modification of test compounds.

Table 1 shows the utility of compounds having Formula I to functionallyinhibit NAMPT.

TABLE 1 TR- FRET TR- Binding - FRET IC50 Binding - (with IC50 PRPP)Example (μM) (μM) 1 0.0921 0.00072 2 0.854 0.0398 3 0.0316 0.000282 40.413 0.000516 5 2.5 0.000684 6 2.91 0.000964 7 0.183 0.000516 8 0.1140.000702 9 1.72 0.000459 10 0.197 0.000457 11 7.6 0.000271 12 0.4860.000292 13 0.653 0.000663 14 0.741 0.00122 15 1.76 0.000841 16 0.4090.000396 17 2.96 0.000401 18 2.73 0.000418 19 2.68 0.000921 20 0.4040.000169 21 0.433 0.000887 22 0.399 0.000277 23 0.281 0.000409 24 0.1670.000363 25 0.508 0.000714 26 0.211 0.0011 27 0.756 0.000658 28 0.1520.00019 29 0.168 0.000236 30 1.18 0.000785 31 0.739 0.000311 32 0.9060.000169 33 0.369 0.000553 34 0.208 0.000377 35 0.387 0.000801 36 0.3560.000444 37 0.129 0.000309 38 0.243 0.000266 39 0.814 0.00026 40 0.04090.000217 41 0.294 0.00115 42 0.697 0.000381 43 4.35 0.000169 44 0.3960.000496 45 0.879 0.00119 46 0.773 0.000318 47 0.0575 0.00062 48 >100.000169 49 0.442 0.000317 50 1.64 0.000817 51 0.264 0.000524 52 0.01860.00579 53 4.45 0.0144 54 0.363 0.00255 55 0.364 0.00137 56 0.1580.00107 57 0.0058 58 0.523 0.00143 59 0.222 0.000695 60 0.00861 0.0014961 0.0782 0.000549 62 0.25 0.000456 63 0.636 0.000283 64 0.518 0.00049565 0.773 0.000685 66 0.558 0.000326 67 0.53 0.000326 68 0.386 0.00047669 0.676 0.000268 70 0.71 0.000616 71 0.754 0.000348 72 0.851 0.00053673 0.605 0.000426 74 0.356 0.000222 75 0.0122 0.000445 76 0.993 0.00073977 0.0561 0.00288 78 0.0565 0.0024 79 0.121 0.00697 80 0.228 0.00571 810.0155 0.00268 82 0.357 0.00642 83 0.899 0.0023 84 1.67 0.0109 85 4.070.00141 86 2.04 0.0119 87 2.05 0.00135 88 2.85 0.00855 89 0.667 0.00038390 0.204 0.00063 91 0.174 0.00126 92 0.183 0.000881 93 0.389 0.00139 940.29 0.000593 95 0.201 0.000991 96 0.192 0.00156 97 0.109 0.000333 980.12 0.000367 99 0.119 0.000411 100 0.102 0.000169 101 0.332 0.00173 1020.385 0.00121 103 0.84 0.00144 104 0.135 0.002 105 0.106 0.000476 1060.247 0.000201 107 0.0451 0.000492 108 1.77 0.00105 109 0.34 0.000209110 0.423 0.000174 111 0.263 0.000209 112 0.0465 0.000169 113 0.3560.000169 114 0.818 0.00111 115 0.243 0.000676 116 0.863 0.00069 1170.392 0.000436 118 0.0352 0.000234 119 0.942 0.000783 120 0.07390.000367 121 0.486 0.000234 122 0.255 0.00476 123 0.133 0.00257 124 1.10.00212 125 0.547 0.00209 126 0.102 0.000963 127 0.0522 0.000522 1280.0307 0.000873 129 0.0116 0.000634 130 0.0532 0.000981 131 0.01520.00167 132 0.155 0.0133 133 0.067 0.000709 134 0.303 0.00149 135 0.07380.00127 136 0.0727 0.000512 137 0.315 0.00721 138 0.0807 0.000424 1390.582 0.000173 140 1.34 0.000927 141 2.11 0.000757 142 1.43 0.00305 1438.71 0.00203 144 9.49 0.00292 145 0.191 0.00108 146 0.261 0.000403 1470.251 0.00063 148 6.23 0.00135 149 >10 0.00486 150 6.11 0.00349 151 7.150.00554 152 3.6 0.00691 153 0.118 0.00188 154 0.194 0.0026 155 3.370.0023 156 3.27 0.00318 157 4.14 0.0011 158 0.341 0.00639 159 2.490.00216 160 3.22 0.00126 161 1.31 0.00289 162 2.57 0.00209 163 2.10.00629 164 2.46 0.00346 165 1.53 0.00161 166 1.43 0.00181 167 1.730.00252 168 1.11 0.000951 169 0.375 0.00425 170 3.36 0.00225 171 2.170.00251 172 2.21 0.00355 173 1.51 0.00124 174 0.0283 0.000169 175 0.6970.0009 176 0.0606 0.000414 177 0.0201 0.000169 178 0.0143 0.000169 1790.0581 0.000445 180 0.584 0.000266 181 0.349 0.000283 182 0.139 0.0004183 1.05 0.0018 184 4.34 0.00254 185 >10 0.00186 186 0.0657 0.000347 1870.549 0.000172 188 >10 0.00509 189 0.192 0.0111 190 0.4 0.00457 1910.821 0.00609 192 0.238 0.000242 193 0.516 0.000266 194 0.0323 0.00024195 0.0247 0.000251 196 0.358 0.000169 197 1.57 0.000505 198 0.03250.000225 199 0.00976 0.000311 200 0.063 0.000482 201 0.0466 0.000281 2020.216 0.000355 203 0.0137 0.00021 204 4.83 0.000773 205 1.06 0.000358206 0.0257 0.000263 207 1.51 0.000282 208 0.404 0.000169 209 0.8110.000988 210 0.469 0.000363 211 1.66 0.000453 212 0.0448 0.00021 2130.116 0.000271 214 0.641 0.00128 215 2.01 0.00304 216 0.118 0.00019 2170.22 0.0002 218 0.123 0.000169 219 0.0794 0.000903 220 0.0742 0.000278221 0.12 0.000352 222 0.112 0.000192 223 0.109 0.000354 224 0.2330.000555 225 0.155 0.000673 226 0.113 0.000608 227 0.0162 0.000273 2280.0494 0.000238 229 0.0136 0.000398 230 0.294 0.000169 231 0.8170.000546 232 0.396 0.000277 233 0.495 0.000401 234 0.904 0.000736 2350.494 0.000369 236 0.604 0.000243 237 0.451 0.000285 238 0.123 0.000187239 0.308 0.000771 240 7.35 0.00875 241 0.0674 0.000169 242 0.05710.000169 243 0.169 0.000169 244 >10 0.00169 245 2.89 0.000502 246 0.07320.00022 247 0.0627 0.000275 248 0.0658 0.000169 249 0.817 0.00072 2500.0205 0.00023 251 2.2 0.00063 252 0.0374 0.000274 253 0.0144 0.000229254 0.0313 0.000306 255 8.19 0.00222 256 0.126 0.000266 257 0.1010.000344 258 0.113 0.000558 259 0.0266 0.000169 260 0.0465 0.000351 2610.0627 0.000231 262 0.00367 0.000221 263 0.0486 0.000247 264 0.04040.000412 265 0.0331 0.000266 266 0.12 0.000333 267 0.0543 0.000291 2680.755 0.000169 269 0.0412 0.000169 270 0.0609 0.000991 271 0.05170.000169 272 0.0272 0.000417 273 0.0493 0.000555 274 0.0178 0.000196 2750.0123 0.00043 276 0.107 0.000468 277 0.103 0.000667 278 0.102 0.000621279 0.0688 0.000437 280 0.0113 0.000213 281 0.0055 0.000214 282 0.07650.000297 283 0.0632 0.000264 284 0.00796 0.000169 285 0.0826 0.000593286 0.12 0.000412 287 0.0673 0.000351 288 0.0495 0.000568 289 0.1550.000286 290 0.415 0.00096 291 0.159 0.000449 292 1.54 0.00115 2930.0273 0.000169 294 0.0447 0.000169 295 0.0561 0.000292 296 0.0670.000226 297 0.177 0.000286 298 3.41 0.000557 299 0.172 0.000283 3000.0614 0.000169 301 0.288 0.000301 302 0.16 0.000435 303 0.009990.000169 304 0.0662 0.000169 305 0.494 0.000449 306 0.144 0.000169 3070.0508 0.000169 308 0.306 0.000169 309 0.117 0.000169 310 0.564 0.000217311 0.289 0.000274 312 0.165 0.000243 313 0.531 0.00036 314 1.980.000581 315 0.231 0.00032 316 0.0421 0.000169 317 0.317 0.000282 3180.0416 0.000228 319 0.466 0.000192 320 0.0963 0.000208 321 3.16 0.000792322 6.04 0.0341 323 1.4 0.000232 324 0.981 0.000752 325 0.18 0.000278326 2.35 0.0013 327 1.32 0.000558 328 0.068 0.000169 329 0.0308 0.000169330 0.32 0.000432 331 0.383 0.000416 332 0.18 0.000297 333 0.5830.000346 334 0.0809 0.000345 335 0.632 0.000354 336 0.334 0.000264 3370.497 0.000205 338 0.609 0.000394 339 >10 0.000797 340 >10 0.000817341 >10 0.000719 342 >10 0.000454 343 >10 0.000456 344 0.036 0.000169345 0.201 0.00027 346 3.11 0.000548 347 4.73 0.000667 348 >10 0.00152349 4.11 0.000736 350 >10 0.000795 351 8.39 0.000792 352 >10 0.00106 3533.17 0.00047 354 >10 0.000526 355 0.831 0.000169 356 >10 0.000169357 >10 0.000291 358 1.84 0.00219 359 >10 0.0025 360 0.291 0.000717 3615.03 0.00194 362 0.143 0.000256 363 0.588 0.000305 364 0.135 0.000172365 1.34 0.000171 366 0.146 0.000435 367 0.65 0.00018 368 0.602 0.000317369 0.429 0.000337 370 0.0476 0.000175 371 1.44 0.000298 372 2.440.00046 373 3.04 0.00036 374 1.67 0.000292 375 0.986 0.000241 376 1.050.000305 377 1.67 0.000275 378 0.897 0.000169 379 0.279 0.00029 3800.179 0.000251 381 0.0841 0.000259 382 0.119 0.000204 383 0.04950.000225 384 0.406 0.000375 385 0.491 0.000539 386 0.283 0.000254 3870.419 0.000467 388 0.388 0.000506 389 0.584 0.000617 390 0.133 0.000445391 0.171 0.000227 392 0.814 0.000465 393 >10 0.00437 394 >10 0.00308395 0.0125 0.000193 396 0.0226 0.00036 397 0.0177 0.000169 398 0.210.000792 399 9.5 0.00154 400 0.0812 0.000298 401 0.0126 0.000292 4020.0548 0.000327 403 1.55 0.000847 404 2.55 0.00088 405 0.0784 0.000214406 1.14 0.000505 407 0.22 0.000659 408 0.276 0.000725 409 >10 0.48 4100.0207 0.000169 411 1.87 0.000556 412 1.25 0.000424 413 0.805 0.000279414 2.63 0.000307 415 1.62 0.000246 416 2.5 0.000318 417 6.84 0.000264418 4.75 0.000233 419 2.43 0.000197 420 2.71 0.000226 421 2.45 0.000271422 1.72 0.000212 423 8.26 0.000338 424 0.988 0.000494 425 0.1530.000227 426 0.0256 0.000169 427 0.15 0.00027 428 0.0871 0.000258 4290.129 0.000396 430 0.292 0.000264 431 0.301 0.000276 432 0.304 0.00033433 0.2 0.000248 434 0.102 0.000169 435 0.163 0.000191 436 1.59 0.000416437 0.0291 0.000169 438 0.145 0.000427 439 0.453 0.000641 440 0.2950.00049 441 0.338 0.000324 442 0.301 0.0002 443 0.138 0.000274 444 0.1560.000244 445 0.11 0.000212 446 0.388 0.000253 447 0.261 0.000232 4480.175 0.000176 449 0.256 0.000169 450 0.422 0.000244 451 0.4 0.000373452 0.293 0.000285 453 0.152 0.000258 454 0.405 0.00034 455 0.01670.000194 456 0.389 0.000169 457 1.14 0.000487 458 0.94 0.000382 4590.381 0.00041 460 0.569 0.000307 461 0.459 0.000169 462 0.0591 0.000266463 0.314 0.000529 464 0.0634 0.000169 465 0.0138 0.000169 466 0.07490.000287 467 0.0911 0.000278 468 >10 0.000985 469 >10 0.000432 470 5.580.000456 471 3.44 0.000471 472 2.86 0.000334 473 >10 0.00101 474 1.980.000362 475 0.00976 0.000169 476 0.0708 0.000194 477 0.0729 0.000235478 0.192 0.00024 479 0.063 0.000243 480 0.181 0.000342 481 0.05720.000176 482 0.0763 0.000259 483 0.13 0.000575 484 0.0795 0.00019 4850.0956 0.000205 486 0.0917 0.000232 487 0.143 0.000334 488 0.1380.000544 489 1.22 0.000263 490 0.753 0.000267 491 >10 0.0019 492 >100.000863 493 1.29 0.000455 494 7.56 0.000712 495 1.47 0.000399 496 0.1990.00114 497 0.0242 0.00286 498 0.309 0.000169 499 0.113 0.00038 5000.181 0.000169 501 0.104 0.000483 502 0.169 0.000385 503 0.0532 0.000277504 0.185 0.000361 505 0.253 0.000355 506 0.245 0.000407 507 0.1210.000359 508 0.257 0.000481 509 0.163 0.000384 510 0.142 0.000284 5110.0653 0.000286 512 0.631 0.000209 513 0.0239 0.000188 514 0.3680.000249 515 0.18 0.000268 516 0.117 0.000266 517 0.33 0.000264 5180.234 0.000169 519 0.218 0.000338 520 0.565 0.000301 521 0.413 0.000292522 0.0581 0.000199 523 0.343 0.000422 524 0.0247 0.000169 525 0.08640.000213 526 0.126 0.000275 527 0.141 0.000265 528 0.126 0.000276 5290.248 0.000283 530 0.378 0.000791 531 0.333 0.000253 532 0.338 0.000178533 0.101 0.000169 534 0.145 0.000251 535 0.297 0.000325 536 0.07760.000202 537 0.461 0.00023 538 0.275 0.000514 539 0.0985 0.00031 5400.266 0.000305 541 0.175 0.000448 542 0.0351 0.000337 543 1.48 0.000383544 0.871 0.000437 545 0.109 0.000403 546 0.237 0.0232 547 0.4980.000423 548 0.397 0.000471 549 0.0812 0.000224 550 0.762 0.000427 5510.713 0.000392 552 0.184 0.000543 553 0.478 0.000592 554 0.451 0.000837555 0.427 0.000749 556 0.00543 0.000407 557 0.167 0.000359 558 1.410.000352 559 0.681 0.000223 560 0.969 0.000312 561 0.869 0.000335 5620.218 0.000607 563 0.322 0.00419 564 0.0238 0.00343 565 0.215 0.00538566 >10 0.216 567 0.403 0.00111 568 0.375 0.000723 569 0.217 0.000669570 0.0704 0.000751 571 0.0417 0.000494 572 0.0516 0.000403 573 0.02420.000403 574 0.0975 0.000505 575 3.25 0.0108 576 0.016 0.000783 5770.0189 0.000361 578 0.682 0.000775 579 0.488 0.000634 580 1.47 0.000798581 0.945 0.00109 582 0.711 0.000911 583 1.12 0.000799 584 0.8110.000756 585 0.641 0.000648 586 0.842 0.00109 587 0.236 0.000917 5880.684 0.000623 589 0.0161 0.000887 590 0.666 0.000734 591 0.138 0.000761592 0.0388 0.000603 593 0.767 0.000544 594 0.0227 0.000682 595 0.1330.000746 596 0.691 0.000909 597 0.232 0.000862 598 0.457 0.000804 5990.527 0.000786 600 0.51 0.000169 601 0.712 0.000682 602 0.786 0.000887603 1.03 0.00101 604 0.151 0.000843 605 0.559 0.000886 606 0.2810.000169 607 0.478 0.000796 608 0.481 0.00051 609 0.598 0.00062 6100.751 0.000762 611 0.288 0.000621 612 0.706 0.000919 613 0.347 0.000916614 0.216 0.00067 615 0.544 0.00079 616 0.174 0.00049 617 0.164 0.000645618 0.5 0.000751 619 0.0793 0.000616 620 0.71 0.001 621 0.114 0.00542622 0.0294 0.00236 623 1.01 0.0016 624 0.261 0.000627 625 0.795 0.00076626 0.645 0.000793 627 0.211 0.00071 628 0.706 0.000978 629 0.230.000643 630 0.266 0.000563 631 0.616 0.00126 632 0.27 0.000698 6330.335 0.000707 634 0.353 0.000648 635 0.462 0.000975 636 0.238 0.000915637 0.36 0.000421 638 0.0166 0.000545 639 0.215 0.000713 640 0.170.000817 641 0.0748 0.000684 642 0.454 0.000532 643 0.028 0.000552 6440.0817 0.00069 645 0.091 0.000474 646 0.195 0.00051 647 0.173 0.000672648 0.661 0.00106 649 0.203 0.000749 650 0.153 0.00111 651 0.2760.000715 652 0.535 0.00116 653 0.831 0.000893 654 0.213 0.000945 6550.23 0.000998 656 0.218 0.000738 657 0.232 0.000589 658 0.137 0.00076659 0.646 0.00071 660 0.282 0.000693 661 0.462 0.000641 662 0.3180.000671 663 0.653 0.00107 664 0.214 0.000733 665 0.123 0.000357 6660.193 0.000855 667 0.226 0.000798 668 0.263 0.0011 669 0.407 0.000807670 0.062 0.000545 671 0.611 0.00106 672 0.313 0.000504 673 0.4520.000697 674 0.297 0.000535 675 0.376 0.00207 676 0.126 0.00698 6770.00177 0.000796 678 0.0412 0.00023 679 0.0228 0.00174 680 0.03710.00238 681 0.0276 0.002 682 0.607 0.00158 683 0.154 0.00119 684 0.4810.00134 685 1.25 0.00136 686 0.959 0.0013 687 0.0973 0.00116 688 1.110.00266 689 0.016 0.00132 690 0.0643 0.00122 691 0.169 0.00067 6920.0839 0.00119 693 0.781 0.00142 694 0.163 0.00112 695 0.0137 0.000621696 0.272 0.000725 697 0.735 0.000802 698 0.0364 0.000629 699 0.04110.000721 700 0.0684 0.00103 701 0.367 0.000856 702 0.568 0.00129 7030.559 0.000824 704 0.503 0.000777 705 0.876 0.00163 706 0.0841 0.000937707 0.277 0.000624 708 0.06 0.0009 709 0.0194 0.000473 710 0.04910.00125 711 0.0885 0.00111 712 0.0911 0.000907 713 0.0443 0.000689 7140.168 0.000991 715 0.0659 0.000771 716 0.0502 0.000607 717 0.1860.000428 718 0.0236 0.000755 719 0.00632 0.000835 720 0.0367 0.000181721 0.125 0.00121 722 0.0394 0.00101 723 0.154 0.000932 724 0.1610.000992 725 0.0196 0.000747 726 0.251 0.000534 727 0.166 0.000783 7280.14 0.000496 729 0.428 0.000765 730 0.489 0.000847 731 0.223 0.000391732 0.0213 0.000471 733 0.119 0.000712 734 0.0142 0.000605 735 0.6460.000864 736 3.09 0.00073 737 0.0704 0.000612 738 0.364 0.000705 7390.0377 0.000672 740 0.0701 0.000403 741 0.068 0.000647 742 0.2410.000526 743 0.0633 0.000691 744 1.08 0.000806 745 0.994 0.000783 7460.795 0.000839 747 0.435 0.00175 748 0.558 0.000648 749 0.392 0.00079750 1.53 0.00154 751 1.24 0.001 752 5.19 0.00077 753 0.403 0.000783 7540.00492 0.00051 755 0.013 0.00057 756 0.123 0.000609 757 0.0156 0.000705758 0.132 0.00061 759 0.0285 0.000799 760 0.0289 0.00071 761 0.09440.000394 762 0.0301 0.000506 763 0.0485 0.000478 764 0.135 0.000465 7650.0365 0.000782 766 0.0615 0.000581 767 0.265 0.00064 768 0.02810.000672 769 0.0984 0.000705 770 0.0388 0.000735 771 0.0708 0.000573 7720.0615 0.000828 773 0.0726 0.000773 774 0.103 0.00046 775 0.05190.000538 776 0.0215 0.000169 777 0.0394 0.00092 778 0.0276 0.000414 7790.0142 0.000603 780 0.25 0.000382 781 0.0875 0.000839 782 0.134 0.000466783 0.0644 0.000907 784 0.0226 0.000455 785 0.0236 0.000638 786 0.04440.000484 787 0.055 0.000474 788 0.082 0.000674 789 0.0217 0.000434 7900.0795 0.000586 791 0.0471 0.00115 792 0.116 0.0005 793 0.0231 0.000398794 0.029 0.000465 795 0.0896 0.000764 796 0.0917 0.00049 797 0.09720.000671 798 0.0957 0.00047 799 0.102 0.000406 800 0.0821 0.000925 8010.866 0.001 802 0.0359 0.000533 803 0.314 0.00101 804 0.289 0.000445 8053.92 0.00112 806 2.74 0.000543 807 0.628 0.000509 808 0.0944 0.000568809 0.0953 0.00063 810 0.481 0.0126 811 0.0998 0.00286 812 0.08 0.00257813 0.0112 0.00153 814 0.0687 0.00163 815 0.053 0.00193 816 0.04610.00158 817 0.0658 0.0016 818 1.52 0.000644 819 0.0199 0.000624 8200.499 0.00928 821 0.663 0.000284 822 0.104 0.00346 823 0.189 0.000356824 0.118 0.000566 825 0.0261 0.000538 826 0.00779 0.000897

NAMPT Cell Proliferation Assay

PC3 cells were seeded in 96-well black plates (Corning #3904) at 500cells/well in 90 μl of RPMI media containing 10% heat-inactivated FBSand incubated overnight at 37° C. and 5% CO₂ to allow cells to attach towells. The following day, test compounds were serially diluted in neatDMSO to 1000× final concentrations prior to dilution with RPMI media to10× and 1% DMSO. Ten μL of the 100× compounds were then transferred towells containing cells to produce a dose response of 10-fold dilutionsfrom 10 M to 1×10⁻⁵ M. Cells were incubated for 5 days at 37° C. and 5%CO₂, then cell viability was measured using Cell Titer Glo reagent(Promega #G7571). Percent inhibition values were calculated and fittedto a sigmoidal dose response curves using Assay Explorer software todetermine IC50s. To assess whether inhibition of cell viability was dueto NAMPT inhibition, the proliferation assay was also performed in thepresence of 0.3 mM nicotinamide mononucleotide.

Table 2 shows the results of the cell proliferation assay.

TABLE 2 Cell Titer-Glo - IC50 Example (μM) 1 0.0609 2 >10 3 0.0367 40.935 5 0.74 6 6.65 7 0.527 8 0.0702 9 0.649 10 0.331 11 4.53 12 0.21313 1.17 14 0.644 15 3.97 16 0.325 17 4.96 18 0.36 19 6.63 20 0.102 210.899 22 0.142 23 0.0415 24 0.691 25 0.146 26 0.261 27 7.54 28 0.0142 290.0439 30 0.0384 31 0.107 32 0.284 33 0.0673 34 0.0383 35 0.0586 360.0514 37 0.0347 38 0.0659 39 7.28 40 0.0708 41 0.138 42 1.59 43 7.45 441.58 45 2.07 46 6.28 47 0.0648 48 5.32 49 7.04 50 6.14 51 0.083 520.00407 53 3.3 54 0.303 55 0.0146 56 0.00886 57 0.00576 58 0.0526 590.143 60 0.00958 61 0.00601 62 0.0165 63 0.0168 64 0.0198 65 0.0656 660.0115 67 0.0119 68 0.0538 69 0.0166 70 0.0278 71 0.0667 72 0.0659 730.0595 74 0.014 75 0.00149 76 0.185 77 0.0142 78 0.0407 79 0.00745 800.0194 81 0.0071 82 0.0679 83 0.0243 84 0.762 85 2.61 86 5.72 87 6.58 888.11 89 0.113 90 0.0187 91 0.0139 92 0.00948 93 0.00713 94 0.0142 950.0106 96 0.00965 97 0.00455 98 0.0194 99 0.0264 100 0.0162 101 0.00244102 0.013 103 0.0621 104 0.00846 105 0.00661 106 0.0787 107 0.0108 1087.66 109 0.0522 110 0.202 111 0.0755 112 0.00696 113 0.0933 114 0.142115 0.00638 116 0.0613 117 0.0639 118 0.0182 119 0.146 120 0.0908 1210.00391 122 0.172 123 0.00743 124 0.0208 125 0.023 126 0.00396 1270.00234 128 0.00221 129 0.00274 130 0.00655 131 0.00217 132 0.523 1330.00216 134 0.00654 135 0.00636 136 0.00305 137 0.225 138 0.00383 1390.0122 140 0.0655 141 0.0778 142 0.0182 143 0.0808 144 0.187 145 0.00601146 0.00769 147 0.00669 148 0.0415 149 0.0266 150 0.0362 151 0.0761 1520.0283 153 0.00373 154 0.00667 155 0.0176 156 0.028 157 0.0292 158 0.191159 0.233 160 0.915 161 0.635 162 0.0436 163 0.0964 164 0.101 165 0.137166 0.0971 167 0.104 168 0.208 169 0.0269 170 0.604 171 0.0447 172 0.223173 0.0501 174 0.00112 175 0.313 176 0.00181 177 0.00169 178 0.00185 1790.00218 180 0.00912 181 0.00775 182 0.00137 183 0.063 184 0.0651 1855.05 186 0.00236 187 0.0341 188 6.29 189 0.0293 190 0.0149 191 0.0143192 0.00185 193 0.0199 194 0.000773 195 0.000966 196 0.00675 197 0.0254198 0.00184 199 0.000539 200 0.00572 201 0.00189 202 0.00488 203 0.00239204 1.62 205 0.483 206 0.00131 207 0.739 208 0.0849 209 0.693 210 0.398211 0.95 212 0.0341 213 0.0397 214 0.289 215 0.686 216 0.00659 2170.00342 218 0.0711 219 0.00559 220 0.00573 221 0.00782 222 0.00408 2230.00708 224 0.023 225 0.00927 226 0.00726 227 0.00628 228 0.00856 2290.00106 230 0.0072 231 0.0351 232 0.00927 233 0.00937 234 0.105 2350.0555 236 0.0138 237 0.0372 238 0.00257 239 0.0177 240 0.651 2410.00848 242 0.00756 243 0.028 244 7.04 245 5.5 246 0.00243 247 0.00134248 0.00242 249 0.0665 250 0.000675 251 1.84 252 0.00191 253 0.000702254 0.000938 255 4.29 256 0.00984 257 0.0152 258 0.0325 259 0.00254 2600.00806 261 0.0051 262 0.00187 263 0.00243 264 0.00669 265 0.00159 2660.606 267 0.665 268 5.54 269 0.0151 270 0.973 271 0.00271 272 0.0156 2730.00235 274 0.0104 275 0.0239 276 0.0381 277 0.0832 278 0.0517 279 0.869280 0.013 281 0.0248 282 0.0447 283 0.145 284 0.107 285 0.301 286 0.0194287 0.0241 288 0.00811 289 0.00933 290 0.0722 291 0.0261 292 7.22 2930.00774 294 0.00188 295 0.0242 296 0.0115 297 0.0358 298 2.37 299 8.64300 0.0287 301 0.0258 302 0.0193 303 0.00179 304 0.0188 305 1.17 3060.0219 307 0.0136 308 0.0295 309 0.0548 310 0.0244 311 0.0191 312 0.065313 0.82 314 0.395 315 0.72 316 0.00634 317 0.542 318 0.0421 319 0.0293320 0.171 321 1.13 322 >10 323 0.175 324 0.0547 325 0.0329 326 0.457 3270.638 328 0.0089 329 0.0124 330 0.0229 331 0.227 332 0.0643 333 0.116334 0.0219 335 0.0976 336 0.139 337 0.533 338 0.081 339 9.18 340 >10 3418.3 342 6.73 343 6.53 344 0.00746 345 0.281 346 7.02 347 8.08 348 >10349 5.51 350 8.17 351 8.11 352 9.8 353 7.51 354 7.49 355 1.94 356 1.02357 6.74 358 2.26 359 8.77 360 0.663 361 >10 362 0.106 363 7.66 3640.031 365 0.332 366 0.0215 367 0.601 368 0.0484 369 0.738 370 0.00993371 0.82 372 0.868 373 0.585 374 0.792 375 >10 376 >10 377 >10 378 >10379 0.37 380 0.04 381 0.0173 382 0.0838 383 0.0133 384 0.0517 385 0.11386 0.0424 387 0.0581 388 0.122 389 0.0783 390 0.0803 391 0.0784 3920.666 393 >10 394 >10 395 0.00634 396 0.0324 397 0.00712 398 0.0736 3997.68 400 0.712 401 0.0559 402 0.00671 403 0.0545 404 9.41 405 0.0221 4060.347 407 1.31 408 0.0192 409 10 410 nd 411 4.72 412 0.978 413 0.19 4140.853 415 0.234 416 0.659 417 0.867 418 0.866 419 0.365 420 0.147 4210.317 422 0.109 423 0.187 424 0.521 425 0.069 426 0.0064 427 0.0622 4280.0675 429 0.0186 430 0.0886 431 0.0719 432 0.0363 433 0.0644 4340.00559 435 0.0204 436 0.762 437 0.00702 438 0.0425 439 0.0375 440 4410.0072 442 0.0707 443 0.00896 444 0.0699 445 0.0229 446 0.0612 4470.0125 448 0.0678 449 0.0236 450 0.0701 451 0.0173 452 0.0592 4530.00921 454 0.0422 455 0.0035 456 0.0496 457 0.194 458 0.183 459 0.0777460 0.0509 461 0.0314 462 0.00743 463 0.234 464 0.00679 465 0.000319 4660.00431 467 0.00402 468 2.93 469 3.38 470 0.936 471 6.51 472 0.963 4737.85 474 0.879 475 0.00692 476 0.00942 477 0.00321 478 0.0312 4790.00808 480 0.00743 481 0.00579 482 0.00222 483 0.0124 484 0.00959 4850.0345 486 0.0233 487 0.0833 488 0.0983 489 >10 490 0.0899 491 7.83 4921.27 493 0.486 494 1.22 495 0.127 496 7.14 497 0.742 498 0.0179 4990.00219 500 0.0217 501 0.00596 502 0.0165 503 0.00421 504 0.0154 5050.0305 506 0.0180018 507 0.0032 508 0.0285902 509 0.00747 510 0.0121 5110.00278 512 0.0179 513 0.0011805 514 0.0308 515 0.0158 516 0.021279 5170.0722 518 0.0348 519 0.0609 520 0.101 521 0.0935 522 0.00673 523 0.0171524 0.00246 525 0.00677 526 0.0603 527 0.0598 528 0.024 529 0.227 5300.0821 531 0.0529 532 0.0927 533 0.0174 534 0.00508 535 0.0285 5360.00304 537 0.0431 538 0.00333 539 0.00347 540 0.074 541 0.0645 5420.00289 543 0.386 544 0.647 545 0.0287 546 2.45 547 0.0255558 5480.0744613 549 0.009417 550 0.1741494 551 0.0550545 552 0.0425577 5530.103 554 0.177 555 0.0332 556 0.00655 557 0.0374 558 1.17 559 0.0943560 0.844 561 0.24 562 0.0709 563 5.14 564 0.211 565 0.891 566 >10 5670.237 568 0.18 569 0.226 570 0.00735 571 0.0229 572 0.00666 573 0.00372574 0.005201 575 >10 576 .000569 577 0.00215 578 4.6 579 0.758 580 0.212581 0.0812 582 0.0332 583 0.189 584 0.0587 585 0.0346 586 0.301 5870.00754 588 0.181 589 0.00131 590 0.189 591 0.0193 592 0.00375 593 0.677594 0.00111 595 0.00693 596 0.257 597 0.0335 598 0.0166 599 0.0523 6000.11 601 0.0567 602 0.0486107 603 0.695 604 0.0101 605 0.0661 606 0.0348607 0.0744 608 0.148 609 0.142 610 0.0744 611 0.0709 612 0.695 613 0.14614 0.00572 615 0.0188 616 0.0326 617 0.0826 618 0.125 619 0.0033 6200.131 621 0.0253 622 0.00706 623 0.446 624 0.329 625 0.226 626 0.0807627 0.0175 628 0.0436 629 0.0652 630 0.0404 631 0.0772 632 0.0323 6330.012 634 0.0835 635 0.05 636 0.0184 637 0.0811 638 0.00261 639 0.0581640 0.05 641 0.00999 642 0.0949 643 0.0069 644 0.00408 645 0.034 6460.13 647 0.00699 648 0.203 649 0.0706 650 0.0583 651 0.0648 652 0.0346653 0.715 654 0.0679 655 0.0688 656 0.0385 657 0.036 658 0.0608 6590.223 660 0.0709 661 0.0672 662 0.0934 663 0.09 664 0.0715 665 0.00728666 0.00518 667 0.0458 668 0.0803 669 0.686 670 0.00992 671 0.684 6720.08 673 0.122 674 0.0324 675 0.0698 676 0.0787 677 6.13E−04 678 0.0151679 0.0109 680 0.629 681 0.145 682 0.771 683 0.0361 684 0.32 685 0.074686 0.0772 687 0.00219 688 5.48 689 0.00721 690 0.0138 691 0.0777 6920.0198 693 0.652 694 0.0247 695 0.00582 696 0.667 697 0.633 698 0.000670699 0.00527 700 0.00325 701 0.0761902 702 0.088 703 0.0903 704 0.0915705 0.0958 706 0.00654 707 0.0741 708 0.00597 709 0.00336 710 0.00276711 0.00325 712 0.0058 713 0.00286 714 0.0174 715 0.00349 716 0.021 7170.0724 718 0.00125 719 0.00237 720 0.00582 721 0.0307 722 0.00388 7230.0716 724 0.0632 725 0.006 726 0.0719 727 0.0582 728 0.021 729 0.0459730 0.0295 731 0.05 732 0.0059 733 0.0202 734 0.000553 735 0.688 7368.36 737 0.00405 738 0.0859 739 0.0676 740 0.00813 741 0.0749 742 0.0105743 0.00681 744 0.505 745 0.632 746 0.116 747 0.942 748 0.0507 749 0.077750 0.794 751 0.755 752 6.66 753 0.0746 754 0.00125 755 0.00249 7560.0189 757 0.000435 758 0.0232 759 0.00165 760 0.00119 761 0.0277 7620.00112 763 0.00231 764 0.0687 765 0.00291 766 0.00636 767 0.0672 7680.000905 769 0.00526 770 0.006 771 0.00347 772 0.0024 773 0.00953 7740.00707 775 0.0609 776 0.0021 777 0.00126 778 0.000896 779 0.000499 7800.0817 781 0.00727 782 0.0247 783 0.0098 784 0.00238 785 0.000839 7860.00751 787 0.00675 788 0.00544 789 0.0694 790 0.0026 791 0.000898 7920.00957 793 0.00102 794 0.000883 795 0.0062 796 0.00465 797 0.00698 7980.00963 799 0.00696 800 0.00621 801 0.0573 802 0.00583 803 0.0176 8040.0497 805 7.82 806 1.4 807 0.1 808 0.0011 809 0.0332 810 0.327 8110.0114 812 0.0388 813 0.00221 814 0.0045 815 0.00589 816 0.00482 8170.00927 818 0.716 819 0.013 820 0.802 821 0.192 822 0.0711 823 0.00462824 0.0124 825 0.00106 826 0.00679 827 0.000625 828 0.00644 829 0.00177830 0.000269 831 0.000886 832 0.0101 833 0.07 834 0.0127 835 0.00395 8360.0683 837 0.00277 838 0.0027 839 0.000607 840 0.00275 841 0.00613 8420.0714 843 0.0172 844 0.0148172 845 0.00389 846 0.0744 847 0.0936 8480.0292 849 0.0636 850 0.054 851 0.133 852 0.00832 853 0.00996 8540.000414 855 0.111 856 0.657 857 0.00155 858 0.00059 859 0.0104 8600.00824 861 0.000574 862 0.000780 863 0.000642 864 0.0672 865 0.000861866 0.000525 867 0.0687 868 0.0869 869 6.87 870 0.994 871 7.3 872 >10873 3.87 874 6.65 875 1.14 876 0.0477 877 >10 878 >10 879 0.0633 8800.75 881 8.49 882 >10 883 0.000220 884 0.000968 885 0.005333 8860.000194 887 0.000214 888 0.000494 889 0.651 890 0.0318 891 0.0872 8920.00676 893 0.000662 894 0.202 895 0.73 896 1.58 897 0.716 898 0.223 8990.181 900 0.0174 901 0.865 902 0.0108 903 0.0352 904 0.282 905 0.000994906 0.00417 907 0.00709 908 0.0112 909 7.21 910 >10 911 0.0425 9120.008725 913 0.0144 914 0.0772 915 0.174 916 0.00673 917 0.00679 9180.233 919 0.101 920 0.00794 921 0.157 922 0.00995 923 0.00458 924 0.018925 0.00206 926 0.00969 927 0.00713 928 0.106 929 0.0247 930 0.00209 9310.00677 932 0.0303 933 0.0717 934 0.00638 935 0.0103 936 0.0325 9370.0809 938 0.00627 939 >10 940 0.000691 941 0.000519 942 0.00102 9430.0244 944 0.00336 945 0.00238 946 0.00594 947 0.00328 948 0.00539 9490.0254 950 0.634 951 0.0639 952 0.0103 953 0.00235 954 0.00276 9550.00256 956 0.00883 957 0.00351 958 0.0214 959 0.00976 960 0.00613 9610.00894 962 0.0161 963 0.0195 964 0.00622 965 0.00831 966 0.00209 9670.00396 968 0.00177 969 0.00636 970 0.0109 971 0.0226 972 0.0289 9730.0218 974 0.0287 975 0.0503 976 0.0349 977 0.00265 978 0.00202 9790.0757 980 0.0294 981 0.00654 982 0.1 983 0.724 984 0.0554 985 0.0283986 0.0214 987 0.543 988 0.0601 989 0.0682 990 0.0179 991 0.0669 9920.584 993 0.074 994 0.0121 995 0.0108 996 0.062 997 0.0194 998 0.123 9990.684 1000 0.0818 1001 0.0953 1002 0.154 1003 0.00496 1004 0.0567 10050.0747 1006 0.0737 1007 0.0373 1008 0.00294 1009 0.0012 1010 0.0058 10110.00197 1012 0.00836 1013 0.00232 1014 0.00207 1015 0.00168 1016 0.002191017 0.00229 1018 0.00164 1019 0.00198 1020 0.000901 1021 0.00111 10220.00293 1023 0.00687 1024 0.00352 1025 0.000808 1026 0.00156 10270.00228 1028 0.00736 1029 0.000272 1030 0.002040 1031 0.00773 10320.00888 1033 0.00197 1034 0.00629 1035 0.00304 1036 0.016 1037 0.007761038 0.00784 1039 0.00687 1040 0.0134 1041 0.00241 1042 0.00359 10430.0104 1044 0.000892 1045 0.00669 1046 0.00461 1047 0.000205 10480.00827 1049 0.00239 1050 0.0234 1051 0.000313 1052 0.0271 1053 0.003411054 0.026 1055 0.00438 1056 0.0013 1057 0.0258 1058 0.00249 1059 0.01641060 0.00229 1061 0.00784 1062 0.017 1063 0.00189 1064 0.00412 10650.00143 1066 0.0057 1067 0.37 1068 0.00577 1069 0.00123 1070 0.0008571071 0.000473 1072 0.00624 1073 0.00388 1074 0.0144 1075 0.00762 10760.0057 1077 0.0691 1078 0.00761 1079 0.0182 1080 0.00341 1081 0.195 10820.00218 1083 0.000920 1084 0.0148 1085 0.0256 1086 0.00993 1087 0.001681088 0.0344 1089 0.00827 1090 0.00542 1091 0.00419 1092 0.0177 10930.565 1094 0.0688 1095 0.00445 1096 0.00207 1097 0.0647 1098 0.009551099 0.0156 1100 0.0087 1101 0.00206 1102 0.00177 1103 0.00424 11040.00696 1105 0.0026 1106 0.0275 1107 0.00226 1108 0.0201 1109 0.009211110 0.111 1111 0.062 1112 0.0164 1113 0.0231 1114 0.0218 1115 0.02121116 0.00619 1117 0.0657 1118 0.00418 1119 0.00667 1120 0.00237 11210.00842 1122 0.00996 1123 0.00711 1124 0.000344 1125 0.00477 11260.00236 1127 0.00299 1128 0.00605 1129 0.00805 1130 0.00296 1131 0.03441132 0.00896 1133 0.001 1134 0.00551 1135 0.00423 1136 0.00302 11370.000277 1138 0.00385 1139 0.00141 1140 0.00584 1141 0.0022 1142 0.00291143 0.0174 1144 0.0096 1145 0.00704 1146 0.00188 1147 0.00283 11480.00272 1149 0.00262 1150 0.0641 1151 0.00778 1152 0.00308 1153 0.001721154 0.17043 1156 0.0354 1157 0.0531 1158 0.00204 1159 0.01740 11600.01630 1161 0.061 1162 0.0618 1163 0.0027 1164 0.158 1165 0.577 11660.0261

Compounds which inhibit NAMPT are useful for treating diseases in whichactivation of NF-KB is implicated. Such methods are useful in thetreatment of a variety of diseases including inflammatory and tissuerepair disorders; particularly rheumatoid arthritis, inflammatory boweldisease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukaemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia.

Involvement of NAMPT in the treatment of cancer is described in WO97/48696. Involvement of NAMPT in immuno-supression is described in WO97/48397. Involvement of NAMPT for the treatment of diseases involvingangiogenesis is described in WO 2003/80054. Involvement of NAMPT for thetreatment of rheumatoid arthritis and septic shock is described in WO2008/025857. Involvement of NAMPT for the prophlaxis and treatment ofischaemia is described in WO 2009/109610.

Cancers include, but are not limited to, hematologic and solid tumortypes such as acoustic neuroma, acute leukemia, acute lymphoblasticleukemia, acute myelogenous leukemia (monocytic, myeloblastic,adenocarcinoma, angiosarcoma, astrocytoma, myelomonocytic andpromyelocytic), acute t-cell leukemia, basal cell carcinoma, bile ductcarcinoma, bladder cancer, brain cancer, breast cancer (includingestrogen-receptor positive breast cancer), bronchogenic carcinoma,Burkitt's lymphoma, cervical cancer, chondrosarcoma, chordoma,choriocarcinoma, chronic leukemia, chronic lymphocytic leukemia, chronicmyelocytic (granulocytic) leukemia, chronic myelogenous leukemia, coloncancer, colorectal cancer, craniopharyngioma, cystadenocarcinoma,dysproliferative changes (dysplasias and metaplasias), embryonalcarcinoma, endometrial cancer, endotheliosarcoma, ependymoma, epithelialcarcinoma, erythroleukemia, esophageal cancer, estrogen-receptorpositive breast cancer, essential thrombocythemia, Ewing's tumor,fibrosarcoma, gastric carcinoma, germ cell testicular cancer,gestational trophobalstic disease, glioblastoma, head and neck cancer,heavy chain disease, hemangioblastoma, hepatoma, hepatocellular cancer,hormone insensitive prostate cancer, leiomyosarcoma, liposarcoma, lungcancer (including small cell lung cancer and non-small cell lungcancer), lymphangioendothelio-sarcoma, lymphangiosarcoma, lymphoblasticleukemia, lymphoma (lymphoma, including diffuse large B-cell lymphoma,follicular lymphoma, Hodgkin's lymphoma and non-Hodgkin's lymphoma),malignancies and hyperproliferative disorders of the bladder, breast,colon, lung, ovaries, pancreas, prostate, skin and uterus, lymphoidmalignancies of T-cell or B-cell origin, leukemia, medullary carcinoma,medulloblastoma, melanoma, meningioma, mesothelioma, multiple myeloma,myelogenous leukemia, myeloma, myxosarcoma, neuroblastoma,oligodendroglioma, oral cancer, osteogenic sarcoma, ovarian cancer,pancreatic cancer, papillary adenocarcinomas, papillary carcinoma,peripheral T-cell lymphoma, pinealoma, polycythemia vera, prostatecancer (including hormone-insensitive (refractory) prostate cancer),rectal cancer, renal cell carcinoma, retinoblastoma, rhabdomyosarcoma,sarcoma, sebaceous gland carcinoma, seminoma, skin cancer, small celllung carcinoma, solid tumors (carcinomas and sarcomas), stomach cancer,squamous cell carcinoma, synovioma, sweat gland carcinoma, testicularcancer (including germ cell testicular cancer), thyroid cancer,Waldenström's macroglobulinemia, testicular tumors, uterine cancer,Wilms' tumor and the like.

Schemes and Experimentals

The following abbreviations have the meanings indicated. ADDP means1,1′-(azodicarbonyl)dipiperidine; AD-mix-3 means a mixture of(DHQD)₂PHAL, K₃Fe(CN)₆, K₂CO₃, and K₂SO₄; 9-BBN means9-borabicyclo(3.3.1)nonane; Boc means tert-butoxycarbonyl; (DHQD)₂PHALmeans hydroquinidine 1,4-phthalazinediyl diethyl ether; DBU means1,8-diazabicyclo[5.4.0]undec-7-ene; DIBAL means diisobutylaluminumhydride; DIEA means diisopropylethylamine; DMAP meansN,N-dimethylaminopyridine; DMF means N,N-dimethylformamide; dmpe means1,2-bis(dimethylphosphino)ethane; DMSO means dimethylsulfoxide; dppbmeans 1,4-bis(diphenylphosphino)-butane; dppe means1,2-bis(diphenylphosphino)ethane; dppf means1,1′-bis(diphenylphosphino)ferrocene; dppm means1,1-bis(diphenylphosphino)methane; EDAC-HCl means1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; Fmoc meansfluorenylmethoxycarbonyl; HATU meansO-(7-azabenzotriazol-1-yl)-N,N′N′N′-tetramethyluroniumhexafluorophosphate; HMPA means hexamethylphosphoramide; IPA meansisopropyl alcohol; MP-BH₃ means macroporous triethylammoniummethylpolystyrene cyanoborohydride; TEA means triethylamine; TFA meanstrifluoroacetic acid; THF means tetrahydrofuran; NCS meansN-chlorosuccinimide; NMM means N-methylmorpholine; NMP meansN-methylpyrrolidine; PPh₃ means triphenylphosphine.

The following schemes are presented to provide what is believed to bethe most useful and readily understood description of procedures andconceptual aspects of this invention. Compounds of this invention may bemade by synthetic chemical processes, examples of which are shownherein. It is meant to be understood that the order of the steps in theprocesses may be varied, that reagents, solvents and reaction conditionsmay be substituted for those specifically mentioned, and that vulnerablemoieties may be protected and deprotected, as necessary.

Schemes

As shown in Scheme 1, compounds of formula (1), wherein R⁴ is asdescribed herein, can be reacted with 4-nitrobenzoic acid in thepresence of a base such as but not limited to N-methylmorpholine, anester activating agent such as but not limited to 1-hydroxybenzotriazolehydrate, and a carboxyl activating agent such as but not limited toN-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, to providecompounds of formula (2). The reaction is typically performed at ambienttemperature in a solvent such as but not limited to dimethylformamide.Compounds of formula (3) can be prepared by reacting compounds offormula (2) with hydrogen in the presence of palladium on carbon.

The reaction is typically performed at ambient temperature in a solventsuch as but not limited to methanol. Compounds of formula (3) can bereacted with compounds of formula (4) wherein X and Z are as describedherein, to provide compounds of formula (5). The reaction is typicallyperformed in the presence of bis(2,5-dioxopyrrolidin-1-yl) carbonate anda base such as but not limited to pyridine. The reaction is typicallyperformed at ambient temperature in a solvent such as but not limited toN-methyl-2-pyrrolidinone.

Alternatively, Compounds of formula (3) can be reacted with compounds offormula (6) wherein X is as described herein, to provide compounds offormula (7). The reaction is typically performed in the presence ofbis(2,5-dioxopyrrolidin-1-yl) carbonate and a base such as but notlimited to pyridine. The reaction is typically performed at ambienttemperature in a solvent such as but not limited toN-methyl-2-pyrrolidinone.

Compounds of formula (8), wherein R^(x) is as described herein forsubstituents on the R³ phenyl, can be reacted with compounds of formula(9), wherein X and Z are as described herein, to provide compounds offormula (10). The reaction is typically performed in the presence of abase such as but not limited to N-methylmorpholine, an ester activatingagent such as but not limited to 1-hydroxybenzotriazole hydrate, and acarboxyl activating agent such as but not limited toN-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride. Thereaction is typically performed at ambient temperature in a solvent suchas but not limited to dimethylformamide.

Similarly, compounds of formula (8), wherein R^(x) is as describedherein for substituents on the R³ phenyl, can be reacted with compoundsof formula (11), wherein X is as described herein, to provide compoundsof formula (12). The reaction is typically performed in the presence ofa base such as but not limited to N-methylmorpholine, an esteractivating agent such as but not limited to 1-hydroxybenzotriazolehydrate, and a carboxyl activating agent such as but not limited toN-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride. Thereaction is typically performed at ambient temperature in a solvent suchas but not limited to dimethylformamide.

As shown in Scheme 3, compounds of formula (13), wherein R³ is asdescribed herein, can be reacted with compounds of formula (11), whereinX is as described herein, in the presence ofbis(2,5-dioxopyrrolidin-1-yl) carbonate and a base such as but notlimited to pyridine to provide compounds of formula (14). The reactionis typically performed at ambient temperature in a solvent such as butnot limited to N-methyl-2-pyrrolidinone.

Alternatively, compounds of formula (13), wherein R³ is as describedherein, can be reacted with compounds of formula (9), wherein X and Zare as described herein, in the presence ofbis(2,5-dioxopyrrolidin-1-yl) carbonate and a base such as but notlimited to pyridine to provide compounds of formula (14). The reactionis typically performed at ambient temperature in a solvent such as butnot limited to N-methyl-2-pyrrolidinone.

2-Bromo-5-thiazolecarboxylic acid can be reacted with compounds offormula (9), N-methylmorpholine, an ester activating agent such as butnot limited to 1-hydroxybenzotriazole hydrate, and a carboxyl activatingagent such as but not limited toN-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, to providecompounds of formula (16). The reaction is typically performed atambient temperature in a solvent such as but not limited todimethylformamide. Compounds of formula (16) can be reacted with aminesof formula (1) wherein R⁴ is as described herein, to provide compoundsof formula (17). The reaction is typically performed at an elevatedtemperature in a solvent such as but not limited to acetonitrile and maybe performed in a microwave oven. Compounds of formula (19), which arerepresentative of the compounds of this invention, can be prepared byreacting compounds of formula (17) with compounds of formula (18),wherein R⁴ is as described herein, in the presence of a base such as butnot limited to diisopropylethylamine. The reaction is typicallyperformed at ambient temperature in a solvent such as but not limited totetrahydrofuran. Alternatively, compounds of formula (17) can be reactedwith amines of formula (4), wherein R⁴ is as described herein, toprovide compounds of formula (20), which are representative of thecompounds of Formula (I). The reaction is typically performed in thepresence of bis(2,5-dioxopyrrolidin-1-yl) carbonate and a base such asbut not limited to pyridine. The reaction is typically performed atambient temperature in a solvent such as but not limited toN-methyl-2-pyrrolidinone.

As shown in Scheme 5, compounds of formula (16), which can be preparedas described in Scheme 4 and wherein X and Z are as described herein,can be reacted with suitable boronic acids (or the equivalent boronicester) of formula (21) wherein R⁴ is as described herein, under Suzukicoupling conditions known to those skilled in the art and widelyavailable in the literature, to provide compounds of formula (22), whichare representative of the compounds of Formula (I).

EXAMPLES

The following examples are presented to provide what is believed to bethe most useful and readily understood description of procedures andconceptual aspects of this invention. Each exemplified compound andintermediate was named using ACD/ChemSketch Version 12.5 (20 Apr. 2011)or (3 Sep. 2012), Advanced Chemistry Development Inc., Toronto,Ontario), or ChemDraw Ver. 9.0.7 (CambridgeSoft, Cambridge, Mass.).

EXPERIMENTALS Example 14-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamideExample 1A N-isopentyl-4-nitrobenzamide

4-Nitrobenzoic acid (0.8 g, 4.79 mmol) and 1-hydroxybenzotriazolehydrate (1.1 g, 7.18 mmol) in dimethylformamide (20 mL) was treated withN-methylmorpholine (1.8 mL, 16.75 mmol) and 3-methylbutan-1-amine (0.724mL, 6.22 mmol) followed by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimidehydrochloride (1.38 g, 7.18 mmol). The reaction mixture was stirred atroom temperature for 17 hours. Water was added and the resultingsuspension was stirred for 2 hours. The suspension was filtered and thesolid collected was washed with water and dried to provide the titlecompound.

Example 1B 4-amino-N-isopentylbenzamide

N-Isopentyl-4-nitrobenzamide (1 g, 4.23 mmol) and methanol (40 ml) wereadded to palladium on carbon (0.200 g, 1.879 mmol) in a 250 mL SSpressure bottle and the mixture was stirred for 6 hours with hydrogen at30 psi and room temperature. The mixture was filtered through a nylonmembrane and concentrated to provide the title compound.

Example 1C4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide

A solution of 4-amino-N-isopentylbenzamide (0.05 g, 0.242mmol),bis(2,5-dioxopyrrolidin-1-yl) carbonate (0.078 g, 0.303 mmol) andpyridine (0.020 ml, 0.242 mmol) in N-methyl-2-pyrrolidinone (0.6 mL) wasstirred at room temperature for 1 hour. Diisopropylethylamine (0.127 ml,0.727 mmol) was added followed by addition of a solution ofimidazo[1,2-a]pyridin-6-amine (0.041 g, 0.279 mmol) inN-methyl-2-pyrrolidinone (0.6 mL) dropwise by syringe over 5 minutes.The reaction mixture was stirred for 16 hours at room temperature andthe mixture was treated with water. The resulting suspension was stirredfor 5 minutes and filtered with water washes. Vacuum drying and reversephase chromatography provided the title compound. ¹H NMR (300 MHz,DMSO-d₆) δ ppm 9.04-8.93 (m, 2H), 8.76 (bs, 1H), 8.24 (t, J=5.5 Hz, 1H),7.96 (s, 1H), 7.79 (d, J=8.7 Hz, 2H), 7.58-7.45 (m, 4H), 7.09 (dd,J=9.6, 2.0 Hz, 1H), 3.33-3.20 (m, 2H), 1.68-1.52 (m, 1H), 1.46-1.35 (m,2H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 366 (M+H)⁺.

Example 24-[(imidazo[1,2-a]pyridin-7-ylcarbamoyl)amino]-N-(3-methylbutyl)benzamide

The title compound was prepared as described in Example 1C, substitutingimidazo[1,2-a]pyridin-7-amine for imidazo[1,2-a]pyridin-6-amine. ¹H NMR(300 MHz, DMSO-d₆) δ ppm 9.04 (m, 2H), 8.42 (dd, J=7.5, 0.6 Hz, 1H),8.25 (t, J=5.5 Hz, 1H), 7.78 (m, 4H), 7.53 (d, J=8.7 Hz, 2H), 7.42 (d,J=1.2 Hz, 1H), 6.90 (dd, J=7.3, 2.1 Hz, 1H), 3.30-3.21 (m, 2H),1.69-1.54 (m, 1H), 1.47-2.36 (m, 2H), 0.91 (d, J=6.5 Hz, 6H); MS(ESI(+)) m/e 366 (M+H)⁺.

Example 32-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamideExample 3A 1-(imidazo[1,2-a]pyridin-6-yl)-3-(4-nitrophenyl)urea

A 0° C. solution of imidazo[1,2-a]pyridin-6-amine (1 g, 7.21 mmol),N-ethyl-N-isopropylpropan-2-amine (2.51 ml, 14.42 mmol) anddimethylformamide (21.85 ml) was treated with a solution of1-isocyanato-4-nitrobenzene (1.313 g, 8.00 mmol) in tetrahydrofuran(10.92 ml) which was added dropwise via syringe over 5 minutes. Thereaction mixture was allowed to stir at room temperature for 6 hours,and water was added. The suspension was filtered with water washes togive the title compound after vacuum drying.

Example 3B 1-(4-aminophenyl)-3-(imidazo[1,2-a]pyridin-6-yl)urea

The title compound was prepared as described in Example 1B, substituting1-(imidazo[1,2-a]pyridin-6-yl)-3-(4-nitrophenyl)urea forN-isopentyl-4-nitrobenzamide.

Example 3C2-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}acetamide

The title compound was prepared as described in Example 1A, substituting1-(4-aminophenyl)-3-(imidazo[1,2-a]pyridin-6-yl)urea for3-methylbutan-1-amine and 2-cyclopentylacetic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆, Temp=90° C.) δ ppm 9.73 (bs, 1H), 8.96(m, 1H), 8.66 (s, 1H), 8.62 (s, 1H), 7.95 (s, 1H), 7.57-7.44 (m, 4H),7.37 (d, J=8.9 Hz, 2H), 7.07 (dd, J=9.6, 2.0 Hz, 1H), 2.29-2.15 (m, 3H),1.82-1.68 (m, 2H), 1.68-1.45 (m, 4H), 1.29-1.07 (m, 2H); MS (ESI(+)) m/e378 (M+H)⁺.

TABLE 1 The following Examples were prepared essentially as described inExample 3, substituting the appropriate carboxylic acid in Example 1C.Some products were purified by flash chromatography while others werepurified by reverse-phase HPLC. Accordingly, some Examples were isolatedas trifluoroacetic acid salts. Ex Name ¹H NMR MS 26 N-{4-[(imidazo[1,2-¹H NMR (400 MHz, DMSO-d₆, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm9.49 (bs, 1H), m/e 380 ylcarbamoyl)amino]phenyl}- 8.84 (m, 1H), 8.44 (m,2H), 7.85 (s, (M + H)⁺ 2-(tetrahydrofuran-3- 1H), 7.52-7.44 (m, 4H),7.39-7.29 yl)acetamide (m, 2H), 7.09 (dd, J = 9.6, 2.1 Hz, 1H),3.83-3.72 (m, 2H), 3.68-3.62 (m, 1H), 3.38-3.33 (m, 1H), 2.57 (m, 1H),2.40-2.33 (m, 2H), 2.08- 1.95 (m, 1H), 1.62-1.52 (m, 1H) 27N-{4-[(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ (ESI(+)) a]pyridin-6-ppm δ 9.81 (s, 1H), 8.98-8.93 (m, m/e 310 ylcarbamoyl)amino]phenyl} 1H),8.70-8.62 (m, 2H), 7.96-7.93 (M + H)⁺ acetamide (m, 1H), 7.53-7.45 (m,4H), 7.41- 7.33 (m, 2H), 7.07 (dd, J = 9.5, 2.0 Hz, 1H), 2.01 (s, 3H) 392-ethoxy-N-{4- ¹H NMR (400 MHz, DMSO-d₆, (ESI(+))[(imidazo[1,2-a]pyridin-6- Temp = 90° C.) δ ppm 9.57 (s, 1H), 8.96 m/e354 ylcarbamoyl)amino]phenyl} (m, 1H), 8.69 (s, 1H), 8.64 (s, 1H), (M +H)⁺ acetamide 7.95 (s, 1H), 7.60-7.48 (m, 4H), 7.42-7.37 (m, 2H), 7.07(dd, J = 9.6, 2.0 Hz, 1H), 4.00 (s, 2H), 3.56 (q, J = 7.0 Hz, 2H), 1.19(t, J = 7.0 Hz, 3H) 40 N-{4-[(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆,) δ(ESI(+)) a]pyridin-6- ppm 9.79 (s, 1H), 8.98-8.93 (m, m/e 394ylcarbamoyl)amino]phenyl}- 1H), 8.67 (s, 1H), 8.63 (s, 1H), 7.97- (M +H)⁺ 2-(tetrahydro-2H-pyran-4- 7.93 (m, 1H), 7.54-7.46 (m, 4H),yl)acetamide 7.40-7.34 (m, 2H), 7.07 (dd, J = 9.5, 2.0 Hz, 1H),3.87-3.79 (m, 2H), 3.34-3.26 (m, 2H), 2.25-2.19 (m, 2H), 2.07-1.91 (m,1H), 1.63-1.54 (m, 2H), 1.31-1.17 (m, 2H) 41 N-{4-[(imidazo[1,2- ¹H NMR(400 MHz, DMSO-d₆, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.35 (bs,1H), m/e 395 ylcarbamoyl)amino]phenyl}- 8.85 (m, 1H), 8.50-8.30 (M, 2H),(M + H)⁺ 2-(morpholin-4- 7.86 (s, 1H), 7.55-7.43 (m, 4H), yl)acetamide7.41-7.34 (m, 2H), 7.09 (dd, J = 9.5, 2.0 Hz, 1H), 3.68-3.60 (m, 4H),3.09 (s, 2H), 2.56-2.51 (m, 4H) 42 N-{4-[(imidazo[1,2- (ESI(+))a]pyridin-6- m/e 384 ylcarbamoyl)amino]phenyl}- (M + H)⁺2-(2-methoxyethoxy)acetamide 43 N-{4-[(imidazo[1,2- (ESI(+))a]pyridin-6- m/e 368 ylcarbamoyl)amino]phenyl}- (M + H)⁺ 3-methoxy-2-methylpropanamide 44 N-{4-[(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 338ylcarbamoyl)amino]phenyl} (M + H)⁺ butanamide 45 4,4,4-trifluoro-N-{4-(ESI(+)) [(imidazo[1,2-a]pyridin-6- m/e 392 ylcarbamoyl)amino]phenyl}(M + H)⁺ butanamide 46 -{4-[(imidazo[1,2-a]pyridin- (ESI(+))6-ylcarbamoyl)amino]phenyl} m/e 380 tetrahydro-2H-pyran-4- (M + H)⁺carboxamide 47 N-{4-[(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 366ylcarbamoyl)amino]phenyl}- (M + H)⁺ 4-methylpentanamide 48N-{4-[(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 393ylcarbamoyl)amino]phenyl}- (M + H)⁺ 1-methylpiperidine-4- carboxamide 49N-{4-[(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 428ylcarbamoyl)amino]phenyl} (M + H)⁺ tetrahydro-2H-thiopyran-4-carboxamide 1,1-dioxide 50 N-{4-[(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e382 ylcarbamoyl)amino]phenyl}- (M + H)⁺ 1,4-dioxane-2-carboxamide

Example 44-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenylethyl)benzamideExample 4A methyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate

The title compound was prepared as described in Example 3A, substitutingmethyl 4-isocyanatobenzoate for 1-isocyanato-4-nitrobenzene.

Example 4B 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoic acid

A solution of methyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate (2.1g, 6.77 mmol) in tetrahydrofuran (18.05 ml) and methanol (9.02 ml) wastreated with 2N lithium hydroxide (13.53 ml, 27.1 mmol) and the reactionwas allowed to stir at room temperature for 16 hours. The mixture wasconcentrated, redissolved in 225 mL water and acidified to -pH 4 with 3Nhydrochloric acid. The suspension was filtered with water washes to givethe title compound after vacuum drying.

Example 4C4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]-N-(2-phenylethyl)benzamide

The title compound was prepared as described in Example 1A, substituting2-phenylethanamine for 3-methylbutan-1-amine and4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (500 MHz, DMSO-d₆/D₂O, Temp=90° C.) δ ppm 9.33 (dd, J=1.9,0.8 Hz, 1H), 8.32 (d, J=1.8 Hz, 1H), 8.05 (d, J=2.0 Hz, 1H), 7.90 (d,J=9.7 Hz, 1H), 7.85-7.74 (m, 3H), 7.61-7.51 (m, 2H), 7.35-7.20 (m, 5H),3.49 (dd, J=8.1, 6.9 Hz, 2H), 2.94-2.79 (m, 2H); MS (ESI(+)) m/e 400(M+H)⁺.

TABLE 2 The following Examples were prepared essentially as described inExample 4, substituting the appropriate amine in Example 4C. Someproducts were purified by flash chromatography while others werepurified by reverse-phase HPLC. Accordingly, some Examples were isolatedas trifluoroacetic acid salts. Ex Name ¹H NMR MS 5 4-[(imidazo[1,2- ¹HNMR (500 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm9.37 (dd, J = 2.0, 0.9 Hz, m/e 409 ylcarbamoyl)amino]- 1H), 8.36 (d, J =2.1 Hz, 1H), 8.10 (d, J = 2.1 (M + H)⁺ N-[2- Hz, 1H), 7.94 (d, J = 9.6Hz, 1H), 7.88-7.78 (morpholin-4- (m, 3H), 7.71-7.57 (m, 2H), 4.02 (d, J= 11.3 yl)ethyl]benzamide Hz, 2H), 3.66 (dd, J = 16.1, 10.0 Hz, 4H),3.56 (d, J = 11.3 Hz, 2H), 3.33 (t, J = 6.1 Hz, 2H), 3.17 (d, J = 13.5Hz, 2H), 2.70 (s, 2H) 6 N-(1-hydroxy-2- ¹H NMR (500 MHz, DMSO-d₆/D₂O,(ESI(+)) methylpropan-2- Temp = 90° C.) δ ppm 9.36 (t, J = 6.6 Hz, 1H),m/e 368 yl)-4- 8.34 (d, J = 1.9 Hz, 1H), 8.09 (dd, J = 10.9, 5.4 (M +H)⁺ [(imidazo[1,2- Hz, 1H), 7.90 (t, J = 10.7 Hz, 1H), 7.85-7.73a]pyridin-6- (m, 3H), 7.56 (dd, J = 12.5, 5.6 Hz, 2H), 3.51 (s,ylcarbamoyl)ami- 2H), 1.49-1.23 (m, 6H) no]benzamide 7 N-benzyl-4- ¹HNMR (500 MHz, DMSO-d₆/D₂O, (ESI(+)) [(imidazo[1,2- Temp = 90° C.) δ ppm9.38-9.29 (m, 1H), 8.33 m/e 386 a]pyridin-6- (d, J = 2.0 Hz, 1H), 8.07(d, J = 2.0 Hz, 1H), (M + H)⁺ ylcarbamoyl)ami- 7.96-7.85 (m, 3H), 7.77(td, J = 9.4, 1.5 Hz, no]benzamide 1H), 7.66-7.51 (m, 2H), 7.38-7.31 (m,4H), 7.32-7.19 (m, 1H), 4.48 (s, 2H) 8 N-(cyclopentylmethyl)- ¹H NMR(500 MHz, DMSO-d₆/D₂O, (ESI(+)) 4-[(imidazo[1,2- Temp = 90° C.) δ ppm9.41-9.31 (m, 1H), 8.34 m/e 378 a]pyridin-6- (d, J = 2.0 Hz, 1H), 8.07(d, J = 2.0 Hz, 1H), (M + H)⁺ ylcarbamoyl)ami- 7.91 (d, J = 8.9 Hz, 1H),7.86-7.73 (m, 3H), no]benzamide 7.63-7.51 (m, 2H), 3.19 (d, J = 7.4 Hz,2H), 2.24-2.01 (m, 1H), 1.68 (dt, J = 11.6, 7.2 Hz, 2H), 1.64-1.57 (m,2H), 1.57-1.42 (m, 2H), 1.37-1.14 (m, 2H) 9 4-[(imidazo[1,2- ¹H NMR (500MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.36 (d, J= 1.4 Hz, 1H), m/e 421 ylcarbamoyl)amino]- 8.35 (d, J = 2.0 Hz, 1H),8.10 (d, J = 2.1 Hz, (M + H)⁺ N-[3-(piperidin-1- 1H), 7.94 (d, J = 9.7Hz, 1H), 7.88-7.80 (m, yl)propyl]benzamide 3H), 7.66-7.53 (m, 2H), 3.44(d, J = 12.2 Hz, 2H), 3.34 (t, J = 6.6 Hz, 2H), 3.12-3.02 (m, 2H),2.97-2.85 (m, 2H), 2.02-1.81 (m, 4H), 1.81-1.58 (m, 4H), 1.51-1.31 (m,1H) 10 4-[(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆/D₂O, (ESI(+))a]pyridin-6- Temp = 90° C.) δ ppm 9.36 (dd, J = 6.3, 5.4 Hz, m/e 411ylcarbamoyl)amino]- 1H), 8.35 (d, J = 2.1 Hz, 1H), 8.09 (d, J = 2.0 (M +H)⁺ N-(2- Hz, 1H), 7.92 (d, J = 9.8 Hz, 1H), 7.89-7.80phenoxyethyl)benz- (m, 3H), 7.63-7.55 (m, 2H), 7.30 (dd, J = 8.4, amide7.4 Hz, 2H), 6.95 (dd, J = 11.9, 7.8 Hz, 3H), 4.12 (t, J = 5.8 Hz, 2H),3.64 (t, J = 5.8 Hz, 2H) 11 4-[(imidazo[1,2- ¹H NMR (500 MHz,DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.34 (s, 1H),8.34 (d, J = m/e 393 ylcarbamoyl)amino]- 2.0 Hz, 1H), 8.09 (d, J = 2.0Hz, 1H), 7.92 (d, J = (M + H)⁺ N-[2- 9.1 Hz, 1H), 7.88-7.78 (m, 3H),7.59 (dd, J = (pyrrolidin-1- 16.4, 8.7 Hz, 2H), 3.59 (dd, J = 15.8, 9.8Hz, yl)ethyl]benzamide 4H), 3.33 (t, J = 6.0 Hz, 2H), 3.07 (d, J = 11.0Hz, 2H), 2.05 (s, 2H), 1.97-1.74 (m, 2H) 12 -[(imidazo[1,2- ¹H NMR (500MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.35 (d, J= 1.3 Hz, 1H), m/e 382 ylcarbamoyl)amino]- 8.34 (d, J = 2.0 Hz, 1H),8.08 (d, J = 2.0 Hz, (M + H)⁺ N-[2-(propan-2- 1H), 7.92 (d, J = 9.7 Hz,1H), 7.88-7.77 (m, yloxy)ethyl]benz- 3H), 7.63-7.52 (m, 2H), 3.64-3.55(m, 1H), amide 3.51 (dd, J = 20.1, 13.7 Hz, 2H), 3.39 (t, J = 6.2 Hz,2H), 1.09 (d, J = 6.1 Hz, 6H) 13 N-(2-hydroxy-2- ¹H NMR (500 MHz,DMSO-d₆/D₂O, (ESI(+)) methylpropyl)-4- Temp = 90° C.) δ ppm 9.37-9.31(m, 1H), 8.33 m/e 368 [(imidazo[1,2- (d, J = 1.9 Hz, 1H), 8.06 (d, J =2.0 Hz, 1H), (M + H)⁺ a]pyridin-6- 7.96-7.88 (m, 1H), 7.88-7.81 (m, 2H),7.76 ylcarbamoyl)ami- (dd, J = 9.6, 1.9 Hz, 1H), 7.65-7.53 (m, 2H),no]benzamide 3.27 (s, 2H), 1.15 (d, J = 27.1 Hz, 6H) 14N-[2-hydroxy-1-(4- ¹H NMR (500 MHz, DMSO-d₆/D₂O, (ESI(+))methoxyphenyl)eth- Temp = 90° C.) δ ppm 9.40-9.32 (m, 1H), 8.34 m/e 446yl]-4- (d, J = 2.0 Hz, 1H), 8.08 (d, J = 2.1 Hz, 1H), (M + H)⁺[(imidazo[1,2- 7.95-7.86 (m, 3H), 7.81-7.75 (m, 1H), 7.61- a]pyridin-6-7.55 (m, 2H), 7.39-7.26 (m, 2H), 6.92-6.86 ylcarbamoyl)ami- (m, 2H),5.09-4.96 (m, 1H), 3.72-3.67 (m, no]benzamide 5H), 3.66-3.60 (m, 1H) 154-[(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6-Temp = 90° C.) δ ppm 9.41-9.33 (m, 1H), 8.35 m/e 407 ylcarbamoyl)amino]-(d, J = 2.0 Hz, 1H), 8.09 (d, J = 2.1 Hz, 1H), (M + H)⁺ N-[2-(2- 7.92(d, J = 9.7 Hz, 1H), 7.82-7.72 (m, 3H), oxopyrrolidin-1- 7.63-7.51 (m,2H), 3.50-3.30 (m, 6H), 2.20 yl)ethyl]benzamide (t, J = 8.1 Hz, 2H),1.96-1.86 (m, 2H) 16 4-[(imidazo[1,2- NMR (500 MHz, DMSO-d₆/D₂O, Temp =90° C.) (ESI(+)) a]pyridin-6- δ ppm 9.39-9.29 (m, 1H), 8.34 (d, J = 2.0Hz, m/e 380 ylcarbamoyl)amino]- 1H), 8.08 (d, J = 2.0 Hz, 1H), 7.92 (d,J = 9.5 (M + H)⁺ N-(tetrahydrofuran- Hz, 1H), 7.86-7.77 (m, 3H),7.63-7.53 (m, 2-ylmethyl)benzamide 2H), 3.99 (p, J = 6.3 Hz, 1H), 3.64(dd, J = 14.3, 7.5 Hz, 2H), 3.42-3.24 (m, 2H), 2.03-1.87 (m, 1H),1.89-1.75 (m, 2H), 1.66-1.52 (m, 1H) 17 4-[(imidazo[1,2- ¹H NMR (500MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.34 (d, J= 1.3 Hz, 1H), m/e 338 ylcarbamoyl)amino]- 8.34 (d, J = 2.0 Hz, 1H),8.07 (d, J = 2.0 Hz, (M + H)⁺ N-propylbenzamide 1H), 7.91 (d, J = 9.6Hz, 1H), 7.87-7.73 (m, 3H), 7.64-7.50 (m, 2H), 3.22 (t, J = 7.1 Hz, 2H),1.61-1.45 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 18 4-[(imidazo[1,2- ¹H NMR(500 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.35(d, J = 1.2 Hz, 1H), m/e 423 ylcarbamoyl)amino]- 8.35 (d, J = 2.1 Hz,1H), 8.10 (d, J = 2.1 Hz, (M + H)⁺ N-[3- 1H), 7.93 (d, J = 9.7 Hz, 1H),7.85-7.78 (m, (morpholin-4- 3H), 7.65-7.56 (m, 2H), 4.07-3.96 (m, 2H),yl)propyl]benzamide 3.66 (t, J = 12.1 Hz, 2H), 3.44 (d, J = 12.4 Hz,2H), 3.35 (t, J = 6.6 Hz, 2H), 3.21-3.12 (m, 2H), 3.07 (d, J = 9.4 Hz,2H), 2.03-1.83 (m, 2H) 19 4-[(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆/D₂O,(ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.30 (s, 1H), 8.29 (d, J =m/e 372 ylcarbamoyl)amino]- 1.6 Hz, 1H), 8.02-7.92 (m, 3H), 7.87 (d, J =(M + H)⁺ N-phenylbenzamide 9.6 Hz, 1H), 7.79-7.66 (m, 3H), 7.65-7.58 (m,2H), 7.42-7.33 (m, 2H), 7.20-7.05 (m, 1H) 20 4-[(imidazo[1,2- ¹H NMR(500 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm9.39-9.29 (m, 1H), 8.43- m/e 366 ylcarbamoyl)amino]- 8.29 (m, 1H),8.09-8.03 (m, 1H), 7.96-7.89 (M + H)⁺ N-(2- (m, 1H), 7.87-7.75 (m, 3H),7.66-7.50 (m, methylbutyl)benz- 2H), 3.25-3.16 (m, 1H), 3.14-3.03 (m,1H), amide 1.70-1.58 (m, 1H), 1.48-1.36 (m, 1H), 1.23- 1.05 (m, 1H),0.97-0.79 (m, 6H) 21 4-[(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆/D₂O,(ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.44-9.30 (m, 1H), 8.34 m/e421 ylcarbamoyl)amino]- (t, J = 5.8 Hz, 1H), 8.13-8.05 (m, 1H), 7.92 (d,(M + H)⁺ N-[3-(2- J = 9.7 Hz, 1H), 7.87-7.76 (m, 3H), 7.68-oxopyrrolidin-1- 7.51 (m, 2H), 3.45-3.32 (m, 2H), 3.31-3.14yl)propyl]benzamide (m, 4H), 2.33-2.19 (m, 2H), 2.02-1.87 (m, 2H),1.80-1.63 (m, 2H) 22 4-[(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆/D₂O,(ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.34 (d, J = 1.2 Hz, 1H), m/e394 ylcarbamoyl)amino]- 8.33 (d, J = 2.0 Hz, 1H), 8.07 (d, J = 2.0 Hz,(M + H)⁺ N-(tetrahydro- 1H), 7.91 (d, J = 9.6 Hz, 1H), 7.85-7.75 (m,2H-pyran-4- 3H), 7.62-7.53 (m, 2H), 3.85 (dd, J = 11.4, 2.5ylmethyl)benzamide Hz, 2H), 3.27 (td, J = 11.7, 1.9 Hz, 2H), 3.16 (d, J= 6.9 Hz, 2H), 1.80 (tt, J = 11.3, 3.9 Hz, 1H), 1.59 (d, J = 11.0 Hz,2H), 1.20 (qd, J = 12.0, 4.5 Hz, 2H) 23 4-[(imidazo[1,2- ¹H NMR (500MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6- Temp = 90° C.) δ ppm 9.43-9.28(m, 1H), 8.34 m/e 394 ylcarbamoyl)amino]- (d, J = 2.0 Hz, 1H), 8.08 (d,J = 2.0 Hz, 1H), (M + H)⁺ N-(tetrahydro- 7.92 (d, J = 9.7 Hz, 1H),7.87-7.74 (m, 3H), 2H-pyran-2- 7.65-7.51 (m, 2H), 3.87 (dd, J = 10.6,2.6 Hz, ylmethyl)benzamide 1H), 3.48-3.41 (m, 1H), 3.33 (td, J = 11.1,3.3 Hz, 1H), 3.29-3.21 (m, 2H), 1.78 (d, J = 5.1 Hz, 1H), 1.61 (d, J =12.8 Hz, 1H), 1.54-1.38 (m, 3H), 1.18 (qd, J = 12.1, 3.7 Hz, 1H) 24N-[(1,1- (ESI(+)) dioxidotetrahydro- m/e 428 thiophen-3- (M + H)⁺yl)methyl]-4- [(imidazo[1,2- a]pyridin-6- ylcarbamoyl)ami- no]benzamide

Example 25 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminophenyl)-5,6-dihydropyridine-1 (2H)-carboxylate for4-amino-N-isopentylbenzamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.96 (m,1H), 8.82-8.75 (m, 1H), 8.65 (m, 1H), 7.96 (s, 1H), 7.52-7.36 (m, 6H),7.12-7.04 (m, 1H), 6.12-6.05 (m, 1H), 4.07-3.92 (m, 2H), 3.59-3.49 (m,2H), 2.44 (m, 2H), 1.43 (s, 9H); MS (ESI(+)) m/e 434 (M+H)⁺.

Example 281-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}ureaExample 28A1-(imidazo[1,2-a]pyridin-6-yl)-3-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)urea

A solution of tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate(0.57 g, 1.315 mmol) in dichloromethane (5 ml) was treated withtrifluoroacetic acid (0.608 ml, 7.88 mmol) and the reaction mixture wasstirred at room temperature for 4 hours. Concentration provided thetitle compound.

Example 28B1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}urea

The title compound was prepared as described in Example 1A, substituting1-(imidazo[1,2-a]pyridin-6-yl)-3-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)ureafor 3-methylbutan-1-amine and 2-(tetrahydrofuran-3-yl)acetic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.96 (m, 1H), 8.82(bs, 1H), 8.70 (bs, 1H), 7.96 (s, 1H), 7.55-7.35 (m, 6H), 7.08 (dd,J=9.6, 2.0 Hz, 1H), 6.11 (m, 1H), 4.18-4.05 (m, 2H), 3.90-3.79 (m, 1H),3.76-3.57 (m, 4H), 3.35-3.23 (m, 2H), 2.55-2.39 (m, 4H), 2.05-1.95 (m,1H), 1.60-1.42 (m, 1H); MS (ESI(+)) m/e 446 (M+H)⁺.

TABLE 3 The following Examples were prepared essentially as described inExample 28, substituting the appropriate carboxylic acid in Example 28B.Some products were purified by flash chromatography while others werepurified by reverse-phase HPLC. Accordingly, some Examples were isolatedas trifluoroacetic acid salts. Ex Name ¹H NMR MS 29 1-{4-[1-(2-hydroxy-¹H NMR (300 MHz, DMSO-d₆,) δ ppm 9.01- (ESI(+)) 2-methylpropanoyl)- 8.93(m, 1H), 8.84 (bs, 1H), 8.71 (bs, 1H), m/e 420 1,2,3,6- 7.95 (s, 1H),7.53-7.35 (m, 6H), 7.12-7.04 (M + H)⁺ tetrahydropyridin-4- (m, 1H), 6.13(m, 1H), 5.43 (bs, 1H), 4.20- yl]phenyl}-3- 3.95 (m, 2H), 3.31 (m, 2H),2.58-2.45 (m, imidazo[1,2- 2H), 1.34 (s, 6H) a]pyridin-6-ylurea 301-imidazo[1,2- ¹H NMR (300 MHz, methanol-d₄) δ ppm 9.01- (ESI(+))a]pyridin-6-yl-3-{4- 8.81 (m, 1H), 7.82 (bs, 1H), 7.54-7.49 (m, m/e 461[1-(morpholin-4- 2H), 7.48-7.32 (m, 4H), 7.18 (dd, J = 9.6, (M + H)⁺ylacetyl)-1,2,3,6- 2.0 Hz, 1H), 6.09 (m, 1H), 4.31 (d, J = 2.8 Hz,tetrahydropyridin-4- 1H), 4.18 (d, J = 2.9 Hz, 1H), 3.89-3.76 (m,yl]phenyl}urea 2H), 3.71 (m, 4H), 3.38-3.25 (m, 2H), 2.65 (m, 1H),2.61-2.49 (m, 5H) 31 1-{4-[1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.85(ESI(+)) (ethoxyacetyl)- (d, J = 1.9 Hz, 1H), 8.56 (s, 1H), 8.43 (s,1H), m/e 420 1,2,3,6- 7.87 (s, 1H), 7.50-7.40 (m, 4H), 7.38-7.32 (M +H)⁺ tetrahydropyridin-4- (m, 2H), 7.10 (dd, J = 9.4, 2.0 Hz, 1H), 6.09-yl]phenyl}-3- 6.04 (m, 1H), 4.13 (s, 2H), 4.13-4.08 (m, imidazo[1,2-2H), 3.66 (t, J = 5.7 Hz, 2H), 3.51 (q, J = 6.9 a]pyridin-6-ylurea Hz,2H), 2.50-2.45 (m, 2H), 1.14 (t, J = 6.9 Hz, 3H) 32 1-imidazo[1,2- ¹HNMR (300 MHz, DMSO-d₆) δ ppm 8.96 (ESI(+)) a]pyridin-6-yl-3-(4- (d, J =1.9 Hz, 1H), 8.83 (s, 1H), 8.70 (s, 1H), m/e 450 {1-[(2- 7.96 (s, 1H),7.55-7.42 (m, 4H), 7.42-7.34 (M + H)⁺ methoxyethoxy)acetyl]- (m, 2H),7.08 (dd, J = 9.6, 2.0 Hz, 1H), 6.15- 1,2,3,6- 6.05 (m, 1H), 4.24-4.17(m, 2H), 4.12-4.05 tetrahydropyridin-4- (m, 2H), 3.70-3.54 (m, 4H),3.51-3.43 (m, yl}phenyl)urea 2H), 3.25 (s, 3H), 2.57-2.41 (m, 2H) 331-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) (ESI(+))a]pyridin-6-yl-3-{4- δ ppm 8.89-8.84 (m, 1H), 8.59 (s, 1H), 8.47 m/e 432[1-(tetrahydrofuran- (s, 1H), 7.86 (s, 1H), 7.51-7.40 (m, 4H), (M + H)⁺2-ylcarbonyl)- 7.39-7.31 (m, 2H), 7.12-7.08 (m, 1H), 6.10- 1,2,3,6- 6.04(m, 1H), 4.71-4.64 (m, 1H), 4.15 (m, tetrahydropyridin-4- 2H), 3.84-3.68(m, 4H), 2.54-2.44 (m, 2H), yl]phenyl}urea 2.15-1.96 (m, 2H), 1.92-1.81(m, 2H) 34 1-imidazo[1,2- ¹H NMR (300 MHz, methanol-d₄) δ ppm 8.93(ESI(+)) a]pyridin-6-yl-3-{4- (dd, J = 2.0, 1.0 Hz, 1H), 7.82 (s, 1H),7.56- m/e 446 [1-(tetrahydro-2H- 7.47 (m, 2H), 7.47-7.35 (m, 4H),7.22-7.14 (M + H)⁺ pyran-4- (m, 1H), 6.13-6.07 (m, 1H), 4.32-4.16 (m,ylcarbonyl)-1,2,3,6- 2H), 4.03-3.92 (m, 2H), 3.86-3.77 (m, 2H),tetrahydropyridin-4- 3.61-3.46 (m, 2H), 3.12-2.92 (m, 1H), 2.66-yl]phenyl}urea 2.49 (m, 2H), 1.92-1.71 (m, 2H), 1.72- 1.59 (m, 2H) 351-{4-[1-(1,4-dioxan- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) (ESI(+))2-ylcarbonyl)- δ ppm 8.86 (d, J = 1.2 Hz, 1H), 8.61 (bs, 1H), m/e 4481,2,3,6- 8.49 (bs, 1H), 7.87 (s, 1H), 7.52-7.40 (m, (M + H)⁺tetrahydropyridin-4- 4H), 7.38-7.32 (m, 2H), 7.11 (dd, J = 9.6,yl]phenyl}-3- 2.0 Hz, 1H), 6.10-6.04 (m, 1H), 4.37 (dd, J = imidazo[1,2-9.2, 2.9 Hz, 1H), 4.15 (m, 2H), 3.81-3.63 a]pyridin-6-ylurea (m, 7H),3.58-3.45 (m, 1H), 2.56-2.47 (m, 2H) 36 1-imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆, Temp = 90° C.) (ESI(+)) a]pyridin-6-yl-3-(4- δ ppm 8.91-8.87 (m1H), 8.68 (s, 1H), 8.56 m/e 459 {1-[(1- (s, 1H), 7.90 (s, 1H), 7.53-7.44(m, 4H), (M + H)⁺ methylpiperidin-4- 7.41-7.35 (m, 2H), 7.14 (dd, J =9.6, 2.1 Hz, yl)carbonyl]- 1H), 6.14-6.08 (m, 1H), 4.19-4.13 (m, 2H),1,2,3,6- 3.72 (t, J = 5.7 Hz, 2H), 3.17 (m, 1H), 2.85-tetrahydropyridin-4- 2.77 (m, 2H), 2.64-2.48 (m, 2H), 2.20 (s,yl}phenyl)urea 3H), 2.06-1.94 (m, 2H), 1.76-1.60 (m, 4H) 371-(4-{1-[(1,1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.98-8.94 (ESI(+))dioxidotetrahydro- (m, 1H), 8.83 (bs, 1H), 8.70 (s, 1H), 7.97- m/e 4942H-thiopyran-4- 7.94 (m, 1H), 7.55-7.35 (m, 6H), 7.09 (dd, J = (M + H)⁺yl)carbonyl]- 9.6, 2.0 Hz, 1H), 6.15-6.09 (m, 1H), 4.27- 1,2,3,6- 4.20(m, 1H), 4.13-4.06 (m, 1H), 3.79- tetrahydropyridin-4- 3.62 (m, 2H),3.28-3.02 (m, 5H), 2.40-2.60 yl}phenyl)-3- (m, 2H), 2.08-1.94 (m, 4H)imidazo[1,2- a]pyridin-6-ylurea 38 1-imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆, Temp = 90° C.) (ESI(+)) a]pyridin-6-yl-3-{4- δ ppm 8.88-8.83(m, 1H), 8.59 (bs, 1H), m/e 404 [1-(2- 8.47 (bs, 1H), 7.87 (s, 1H),7.50-7.41 (m, (M + H)⁺ methylpropanoyl)- 4H), 7.39-7.33 (m, 2H), 7.11(dd, J = 9.5, 1,2,3,6- 2.0 Hz, 1H), 6.12-6.06 (m, 1H), 4.17-4.11tetrahydropyridin-4- (m, 2H), 3.69 (t, J = 5.7 Hz, 2H), 2.95-2.86yl]phenyl}urea (m, 1H), 2.50 (m, 2H), 1.05 (d, J = 6.7 Hz, 6H)

Example 511-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}ureaExample 51A 4-(1-isobutyl-1H-pyrazol-4-yl)aniline

A suspension of 4-bromoaniline (406 mg, 2.362 mmol),1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(650 mg, 2.60 mmol),[1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II), complexwith dichloromethane (57.9 mg, 0.071 mmol) and sodium carbonate (526 mg,4.96 mmol) in a 6:2:1 mixture of tetrahydrofuran/water/methanol (12 ml)in a microwave vial was subjected to three vacuum/nitrogen purge cycles.The vial was sealed and heated in an oil bath at 85° C. overnight. Themixture was dissolved in a mixture of ethyl acetate (45 ml) and water(20 ml), and the separated aqueous layer was extracted with ethylacetate (20 ml). The combined organic layers were washed with brine (20ml), dried with magnesium sulfate, filtered and concentrated. Normalphase chromatography provided the title compound.

Example 51B1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea

The title compound was prepared as described in Example 1C, substituting4-(1-isobutyl-1H-pyrazol-4-yl)aniline for 4-amino-N-isopentylbenzamide.¹H NMR (400 MHz, CDCl₃) δ 9.18 (s, 2H), 8.49 (s, 1H), 7.73 (s, 1H), 7.64(d, J=10.3 Hz, 2H), 7.56 (s, 1H), 7.42-7.31 (m, 4H), 7.36 (d, J=9.5 Hz,1H), 6.62 (dd, J=9.6, 1.7 Hz, 1H), 3.92 (d, J=7.3 Hz, 2H), 2.23 (hept,J=6.8 Hz, 1H), 0.93 (d, J=6.7 Hz, 6H). MS (ESI)(+)) m/e 375 (M+H)⁺.

Example 524-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamideExample 52A methyl 4-(2-cyclopentylacetamido)benzoate

A solution of methyl 4-aminobenzoate (0.25 g, 1.654 mmol) intetrahydrofuran (8.27 ml) was treated with diisopropylethylamine (0.433ml, 2.481 mmol) and 2-cyclopentylacetyl chloride (0.279 g, 1.902 mmol)and the reaction mixture was stirred at ambient temperature for 2 hours.Concentration and normal phase chromatography provided the titlecompound.

Example 52B 4-(2-cyclopentylacetamido)benzoic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 4-(2-cyclopentylacetamido)benzoate for methyl4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 52C4-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(2-cyclopentylacetamido)benzoic acid for 4-nitrobenzoic acid. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 10.08 (s, 1H), 8.93 (t, J=5.8 Hz, 1H), 8.47 (s,1H), 7.96 (s, 1H), 7.87-7.81 (m, 2H), 7.70-7.64 (m, 2H), 7.57-7.50 (m,2H), 7.24 (dd, J=9.2, 1.7 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 2.36-2.30 (m,2H), 2.29-2.15 (m, 1H), 1.81-1.65 (m, 2H), 1.67-1.38 (m, 4H), 1.39-0.95(m, 2H); MS (ESI(+)) m/e 377 (M+H)⁺.

Example 532-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamideExample 53A 2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-A]pyridin-6-amine (0.768 g, 5.77 mmol) for3-methylbutan-1-amine and 2-bromo-5-thiazolecarboxylic acid (1 g, 4.81mmol) for 4-nitrobenzoic acid.

Example 53B2-(4-cyanobenzylamino)-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide

To a solution of2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide (165 mg,0.511 mmol) in acetonitrile (2553 μl) was added 4-cyanobenzylamine (67.5mg, 0.511 mmol). The mixture was heated in a microwave (BiotageInitiator) at 180° C. for 30 minutes. The heating was repeated againafter another equivalent of 4-cyanobenzylamine was added. The reactionmixture was purified by normal phase chromatography to provide the titlecompound.

Example 53C2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-yl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 52A,substituting 3-methylbutanoyl chloride for 2-cyclopentylacetyl chlorideand2-(4-cyanobenzylamino)-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ 10.75 (s, 1H),9.62 (s, 1H), 8.43 (d, J=1.6 Hz, 1H), 8.32 (s, 1H), 8.11 (s, 1H),7.99-7.89 (m, 2H), 7.82 (dd, J=18.8, 8.3 Hz, 2H), 7.38 (d, J=8.3 Hz,2H), 5.63 (s, 2H), 2.14 (dt, J=13.4, 6.7 Hz, 1H), 0.88 (d, J=6.7 Hz,6H); (APCI(+)) m/e 459 (M+H)⁺.

TABLE 4 The following Examples were prepared essentially as described inExample 53, substituting the appropriate amine in Example 53A, theappropriate amine in 53B and the appropriate acid chloride in Example53C. Some products were purified by flash chromatography while otherswere purified by reverse-phase HPLC. Accordingly, some Examples wereisolated as trifluoroacetic acid salts. Ex Name ¹H NMR MS 54 2-[(4- ¹HNMR (400 MHz, DMSO-d₆) δ 10.75 (s, (APCI(+)) cyanobenzyl)(3- 1H), 9.61(s, 1H), 8.42 (s, 1H), 8.33 (s, 1H), m/e 461 methoxypropanoyl) 8.10 (s,1H), 7.94 (s, 2H), 7.84 (d, J = 8.3 (M + H)⁺ amino]-N- Hz, 3H), 7.40 (d,J = 8.3 Hz, 2H), 5.64 (s, (imidazo[1,2- 2H), 3.64 (t, J = 6.0 Hz, 2H),3.20 (s, 3H), a]pyridin-6-yl)-1,3- 2.89 (t, J = 6.1 Hz, 2H). thiazole-5-carboxamide 55 2-[(4- ¹H NMR (400 MHz, CDCl₃) δ 8.57 (s, 1H), (APCI(+))cyanobenzyl)(3- 8.16 (d, J = 9.5 Hz, 1H), 7.96 (s, 1H), 7.86 m/e 473methylbutanoyl)ami- (d, J = 1.8 Hz, 1H), 7.81 (d, J = 9.6 Hz, (M + H)⁺no]-N-(imidazo[1,2- 1H), 7.75 (s, 1H), 7.63 (d, J = 8.3 Hz, 2H),a]pyridin-6- 7.24 (d, J = 8.3 Hz, 2H), 5.54 (s, 2H), 4.69 ylmethyl)-1,3-(d, J = 6.1 Hz, 2H), 2.39 (d, J = 6.7 Hz, thiazole-5- 2H), 2.30-2.24 (m,1H), 0.94 (d, J = 6.6 carboxamide Hz, 6H) 56 2-[(4- ¹H NMR (400 MHz,methanol-d₄) δ 8.78 (s, (APCI(+)) cyanobenzyl)(3- 1H), 8.20 (d, J = 2.1Hz, 1H), 8.02 (d, J = m/e 475 methoxypropanoyl) 2.1 Hz, 1H), 8.01 (s,1H), 8.00-7.96 (m, (M + H)⁺ amino]-N- 1H), 7.90 (d, J = 9.3 Hz, 1H),7.70 (d, J = (imidazo[1,2- 8.2 Hz, 2H), 7.38 (d, J = 8.2 Hz, 2H), 5.65a]pyridin-6- (s, 2H), 4.66 (s, 2H), 3.73 (t, J = 5.9 Hz, ylmethyl)-1,3-2H), 2.87 (t, J = 5.9 Hz, 2H) thiazole-5- carboxamide 57 2-[(4- ¹H NMR(400 MHz, methanol-d₄) δ 9.22 (APCI(+)) cyanobenzyl)(3- (td, J = 6.4,1.2 Hz, 1H), 8.75 (d, J = 7.0 m/e 475 methoxypropanoyl) Hz, 1H), 8.18(d, J = 2.0 Hz, 1H), 8.08- (M + H)⁺ amino]-N- 7.95 (m, 2H), 7.80 (s,1H), 7.77-7.66 (m, (imidazo[1,2- 2H), 7.47 (dd, J = 7.1, 1.1 Hz, 1H),7.39 (d, a]pyridin-7- J = 8.2 Hz, 2H), 5.66 (s, 2H), 4.73 (d, J =ylmethyl)-1,3- 4.5 Hz, 2H), 3.74 (t, J = 5.9 Hz, 2H), 2.88 thiazole-5-(t, J = 5.8 Hz, 2H) carboxamide 61 N-(imidazo[1,2- ¹H NMR (400 MHz,methanol-d₄) δ 8.79 (s, (APCI(+)) a]pyridin-6- 1H), 8.22 (d, J = 2.1 Hz,1H), 8.08 (s, 1H), m/e 430 ylmethyl)-2-[(3- 8.05-7.96 (m, 2H), 7.90 (d,J = 9.3 Hz, (M + H)⁺ methoxypropanoyl)(3- 1H), 4.67 (d, J = 3.8 Hz, 2H),4.27 (dd, J = methylbutyl)amino]- 9.3, 7.0 Hz, 2H), 3.79 (t, J = 5.9 Hz,2H), 1,3-thiazole-5- 3.36 (s, 3H), 2.98 (t, J = 5.9 Hz, 2H), 1.80-carboxamide 1.67 (m, 1H), 1.67-1.57 (m, 2H), 1.01 (d, J = 6.5 Hz, 6H)121 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ 9.11 (t, J = (APCI(+))a]pyridin-7- 5.9 Hz, 1H), 8.50 (d, J = 7.0 Hz, 1H), m/e 444ylmethyl)-2-[(3- 8.17 (s, 1H), 7.90 (s, 1H), 7.53 (s, 1H), 7.41 (M + H)⁺methoxypropanoyl)(tet- (s, 1H), 6.85 (dd, J = 7.1, 1.5 Hz, 1H), 4.48rahydrofuran-2- (d, J = 5.8 Hz, 2H), 4.39 (d, J = 12.5 Hz,ylmethyl)amino]- 1H), 4.25-4.08 (m, 2H), 3.78 (dd, J = 14.8,1,3-thiazole-5- 6.8 Hz, 1H), 3.66 (t, J = 6.4 Hz, 2H), 3.65- carboxamide3.55 (m, 1H), 3.26 (s, 3H), 3.06 (ddd, J = 17.2, 13.9, 6.4 Hz, 2H), 1.99(dd, J = 12.7, 7.4 Hz, 1H), 1.94-1.86 (m, 1H), 1.86- 1.74 (m, 1H),1.66-1.53 (m, 1H) 123 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O) δppm (ESI(+)) a]pyridin-6- 8.76 (s, 1 H) 8.24 (d, J = 2.14 Hz, 1 H) 8.10m/e 496 ylmethyl)-2-{[(2- (s, 1 H) 8.02 (d, J = 2.14 Hz, 1 H) 7.89 (d,(M + H)⁺ methyl-1,3-thiazol-5- J = 1.22 Hz, 2 H) 7.45 (s, 1 H) 4.57 (s,2 H) yl)acetyl](tetrahydro- 4.50 (d, J = 12.21 Hz, 1 H) 4.42 (d, J =5.80 furan-2- Hz, 1 H) 4.19-4.31 (m, 2 H) 3.78-3.85 ylmethyl)amino}- (m,1 H) 3.63-3.69 (m, 1 H) 3.28-3.29 1,3-thiazole-5- (m, 2 H) 2.62 (s, 3 H)2.01 (s, 1 H) 1.81- carboxamide 1.95 (m, 2 H) 1.60-1.68 (m, 1 H) 124N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O) δ ppm (ESI(+))a]pyridin-6- 8.78 (s, 1 H) 8.26 (d, J = 1.83 Hz, 1 H) 8.10 m/e 496ylmethyl)-2-{[(2- (s, 1 H) 8.05 (d, J = 2.14 Hz, 1 H) 7.90-7.96 (M + H)⁺methyl-1,3-thiazol-4- (m, 2 H) 7.24 (s, 1 H) 4.58 (s, 2 H) 4.47 (dd,yl)acetyl](tetrahydro- 1 H) 4.18-4.37 (m, 4 H) 3.79-3.86 (m, 1 furan-2-H) 3.62-3.69 (m, 1 H) 2.62 (s, 3 H) 1.97- ylmethyl)amino}- 2.06 (m, 1 H)1.80-1.94 (m, 2 H) 1.56- 1,3-thiazole-5- 1.69 (m, 1H) carboxamide 125N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O) δ ppm (ESI(+))a]pyridin-6- 8.70 (s, 1 H) 8.17 (d, J = 1.83 Hz, 1 H) 8.10 m/e 480ylmethyl)-2-{[(3- (s, 1 H) 7.92 (d, J = 1.83 Hz, 1 H) 7.79-7.84 (M + H)⁺methyl-1,2-oxazol-5- (m, 1 H) 7.73-7.85 (m, 1 H) 6.27 (s, 1 H)yl)acetyl](tetrahydro- 4.55 (s, 2 H) 4.35-4.52 (m, 3 H) 4.19- furan-2-4.27 (m, 2 H) 3.77-3.85 (m, 1 H) 3.62- ylmethyl)amino}- 3.69 (m, 1 H)2.23 (s, 3 H) 2.01 (d, J = 2.75 1,3-thiazole-5- Hz, 1 H) 1.80-1.95 (m, 2H) 1.56-1.67 carboxamide (m, 1 H) 126 2-{[3-(3-chloro-1,2- (ESI(+))oxazol-5- m/e 515 yl)propanoyl](tetra- (M + H)⁺ hydrofuran-2-ylmethyl)amino}-N- (imidazo[1,2- a]pyridin-6- ylmethyl)-1,3- thiazole-5-carboxamide 127 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 510ylmethyl)-2-{[3-(3- (M + H)⁺ methoxy-1,2- oxazol-5- yl)propanoyl](tetra-hydrofuran-2- ylmethyl)amino}- 1,3-thiazole-5- carboxamide 1282-{[(3,5-dimethyl- (ESI(+)) 1,2-oxazol-4- m/e 495 yl)acetyl](tetrahydro-(M + H)⁺ furan-2- ylmethyl)amino}-N- (imidazo[1,2- a]pyridin-6-ylmethyl)-1,3- thiazole-5- carboxamide 129 2-{[3-(3,5-dimethyl- (ESI(+))1,2-oxazol-4- m/e 509 yl)propanoyl](tetra- (M + H)⁺ hydrofuran-2-ylmethyl)amino}-N- (imidazo[1,2- a]pyridin-6- ylmethyl)-1,3- thiazole-5-carboxamide 130 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 494ylmethyl)-2-{[3-(1- (M + H)⁺ methyl-1H-pyrazol-4- yl)propanoyl](tetra-hydrofuran-2- ylmethyl)amino}- 1,3-thiazole-5- carboxamide 131N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 511 ylmethyl)-2-{[3-(4- (M +H)⁺ methyl-1,3-thiazol-5- yl)propanoyl](tetra- hydrofuran-2-ylmethyl)amino}- 1,3-thiazole-5- carboxamide 132 N-(imidazo[1,2-(ESI(+)) a]pyridin-6- m/e 468 ylmethyl)-2- (M + H)⁺ [(tetrahydrofuran-2-ylmethyl)(1H- tetrazol-5- ylacetyl)amino]-1,3- thiazole-5- carboxamide133 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 481 ylmethyl)-2-{[3- (M +H)⁺ (1,2-oxazol-5- yl)propanoyl](tetra- hydrofuran-2- ylmethyl)amino}-1,3-thiazole-5- carboxamide 134 N-(imidazo[1,2- (ESI(+)) a]pyridin-6-m/e 467 ylmethyl)-2-[(1,2- (M + H)⁺ oxazol-3- ylacetyl)(tetrahydro-furan-2- ylmethyl)amino]- 1,3-thiazole-5- carboxamide 135N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 481 ylmethyl)-2-{[3- (M + H)⁺(1,2-oxazol-4- yl)propanoyl](tetra- hydrofuran-2- ylmethyl)amino}-1,3-thiazole-5- carboxamide 136 N-(imidazo[1,2- (ESI(+)) a]pyridin-6-m/e 497 ylmethyl)-2- (M + H)⁺ {(tetrahydrofuran-2- ylmethyl)[3-(1,3-thiazol-2- yl)propanoyl]amino}- 1,3-thiazole-5- carboxamide 139N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ 8.79 (s, (APCI(+))a]pyridin-6- 1H), 8.22 (d, J = 2.1 Hz, 1H), 8.08 (s, 1H), m/e 444ylmethyl)-2-[(3- 8.03 (d, J = 2.2 Hz, 1H), 7.98 (d, J = 1.4 Hz, (M + H)⁺methoxypropanoyl)(tet- 1H), 7.91 (d, J = 9.3 Hz, 1H), 4.66 (s, 2H),rahydrofuran-3- 4.31 (qd, J = 14.8, 7.7 Hz, 2H), 3.96 (td, J =ylmethyl)amino]- 8.2, 5.7 Hz, 1H), 3.87-3.71 (m, 3H), 3.651,3-thiazole-5- (qd, J = 8.9, 5.6 Hz, 2H), 3.36 (s, 3H), 3.02carboxamide (dd, J = 10.4, 5.6 Hz, 2H), 2.94-2.81 (m, 1H), 2.05 (dtd, J= 13.5, 8.0, 5.7 Hz, 1H), 1.75 (ddd, J = 12.6, 7.9, 6.5 Hz, 1H) 140N-(imidazo[1,2- ¹H NMR (500 MHz, methanol-d₄) δ 8.79 (s, (APCI(+))a]pyridin-6- 1H), 8.21 (d, J = 1.9 Hz, 1H), 8.09 (s, 1H), m/e 470ylmethyl)-2- 8.03 (d, J = 2.0 Hz, 1H), 8.00 (d, J = 9.3 Hz, (M + H)⁺[(tetrahydrofuran-3- 1H), 7.91 (d, J = 9.2 Hz, 1H), 4.66 (s, 2H),ylmethyl)(tetrahydro- 4.40 (dd, J = 14.8, 7.0 Hz, 1H), 4.28 (dd, J =2H-pyran-4- 14.7, 8.5 Hz, 1H), 4.06-3.94 (m, 3H), ylcarbonyl)amino]-3.77 (dd, J = 15.0, 8.1 Hz, 1H), 3.68 (dd, J = 1,3-thiazole-5- 8.9, 6.3Hz, 1H), 3.60 (dd, J = 8.9, 4.7 Hz, carboxamide 1H), 3.55 (t, J = 11.7Hz, 2H), 3.24 (tt, J = 11.1, 3.7 Hz, 1H), 2.85 (dt, J = 12.1, 3.5 Hz,1H), 2.11-2.01 (m, 1H), 1.93 (ddd, J = 16.1, 12.7, 4.3 Hz, 1H),1.89-1.82 (m, 1H), 1.75 (dt, J = 13.0, 9.9 Hz, 3H) 142 N-(imidazo[1,2-¹H NMR (400 MHz, methanol-d₄) δ 8.79 (s, (APCI(+)) a]pyridin-6- 1H),8.22 (d, J = 2.1 Hz, 1H), 8.08 (s, 1H), m/e 458 ylmethyl)-2-[(3- 8.03(d, J = 2.1 Hz, 1H), 8.00 (dd, J = 9.4, (M + H)⁺ methoxypropanoyl)(tet-1.4 Hz, 1H), 7.91 (d, J = 9.4 Hz, 1H), 4.66 rahydro-2H- (s, 2H), 4.23(d, J = 7.3 Hz, 2H), 4.00- pyran-4- 3.85 (m, 2H), 3.79 (t, J = 5.9 Hz,2H), 3.36 ylmethyl)amino]- (s, 3H), 3.02 (t, J = 5.9 Hz, 2H), 2.26-2.131,3-thiazole-5- (m, 1H), 1.58-1.50 (m, 2H), 1.49-1.36 carboxamide (m,2H) 143 N-(imidazo[1,2- ¹H NMR (500 MHz, methanol-d₄) δ 8.79 (s,(APCI(+)) a]pyridin-6- 1H), 8.21 (d, J = 2.1 Hz, 1H), 8.09 (s, 1H), m/e470 ylmethyl)-2- 8.03 (d, J = 2.0 Hz, 1H), 8.00 (d, J = 9.3 Hz, (M + H)⁺[(tetrahydrofuran-3- 1H), 7.91 (d, J = 9.3 Hz, 1H), 4.67 (s, 2H),ylcarbonyl)(tetra- 4.32-4.23 (m, 2H), 4.08 (t, J = 8.1 Hz,hydro-2H-pyran-4- 1H), 3.94 (qd, J = 9.9, 3.8 Hz, 4H), 3.87ylmethyl)amino]- (dd, J = 14.8, 7.3 Hz, 1H), 3.83-3.74 (m,1,3-thiazole-5- 1H), 3.35 (dd, J = 11.7, 1.9 Hz, 2H), 2.31 carboxamide(dt, J = 15.4, 7.1 Hz, 1H), 2.18 (td, J = 12.9, 6.6 Hz, 2H), 1.53 (t, J= 10.9 Hz, 2H), 1.50- 1.41 (m, 2H) 144 N-(imidazo[1,2- ¹H NMR (500 MHz,methanol-d₄) δ 8.79 (s, (APCI(+)) a]pyridin-6- 1H), 8.21 (d, J = 2.0 Hz,1H), 8.09 (s, 1H), m/e 484 ylmethyl)-2- 8.03 (d, J = 2.1 Hz, 1H), 8.00(dd, J = 9.3, (M + H)⁺ [(tetrahydro-2H- 1.4 Hz, 1H), 7.91 (d, J = 9.3Hz, 1H), 4.66 pyran-4- (s, 2H), 4.27 (d, J = 7.3 Hz, 2H), 4.03-ylcarbonyl)(tetra- 3.97 (m, 2H), 3.93 (dd, J = 11.4, 2.7 Hz,hydro-2H-pyran-4- 2H), 3.62-3.52 (m, 2H), 3.35 (dd, J = 11.6,ylmethyl)amino]- 2.2 Hz, 2H), 3.26 (dd, J = 9.3, 5.6 Hz, 1H),1,3-thiazole-5- 2.21-2.10 (m, 1H), 1.89 (ddd, J = 16.0, carboxamide12.6, 4.4 Hz, 2H), 1.76 (dd, J = 13.0, 1.5 Hz, 2H), 1.54 (dt, J = 7.1,3.0 Hz, 2H), 1.51- 1.42 (m, 2H) 145 N-(imidazo[1,2- ¹H NMR (500 MHz,methanol-d₄) δ 8.78 (s, (APCI(+)) a]pyridin-6- 1H), 8.21 (s, 1H), 8.07(s, 1H), 8.02 (s, 1H), m/e 444 ylmethyl)-2-{(3- 8.00 (d, J = 9.4 Hz,1H), 7.91 (d, J = 9.4 Hz, (M + H)⁺ methoxy- 1H), 4.66 (s, 2H), 4.52 (d,J = 14.9 Hz, 1H), propanoyl)[(2R)- 4.29 (d, J = 6.8 Hz, 1H), 4.17 (dd, J= 14.9, tetrahydrofuran-2- 8.9 Hz, 1H), 3.88 (dd, J = 14.5, 7.2 Hz, 1H),ylmethyl]amino}- 3.76 (dd, J = 14.0, 7.9 Hz, 2H), 3.74-3.691,3-thiazole-5- (m, 1H), 3.36 (s, 3H), 3.13 (q, J = 6.1 Hz, carboxamide2H), 2.10 (td, J = 12.4, 7.4 Hz, 1H), 2.04- 1.94 (m, 1H), 1.94-1.85 (m,1H), 1.67 (dq, J = 15.3, 7.8 Hz, 1H) 146 N-(imidazo[1,2- ¹H NMR (500MHz, methanol-d₄) δ 8.79 (s, (APCI(+)) a]pyridin-6- 1H), 8.21 (s, 1H),8.08 (s, 1H), 8.02 (d, J = m/e 456 ylmethyl)-2- 1.8 Hz, 1H), 8.00 (d, J= 9.4 Hz, 1H), 7.91 (M + H)⁺ {(tetrahydrofuran-3- (d, J = 9.3 Hz, 1H),4.66 (s, 2H), 4.61 (t, J = ylcarbonyl)[(2R)- 13.7 Hz, 1H), 4.30-4.17 (m,2H), 4.06 tetrahydrofuran-2- (ddd, J = 15.8, 14.9, 7.9 Hz, 1H), 3.99-ylmethyl]amino}- 3.91 (m, 2H), 3.90-3.79 (m, 3H), 3.76- 1,3-thiazole-5-3.68 (m, 1H), 2.32 (qd, J = 12.8, 6.7 Hz, carboxamide 1H), 2.25-2.04 (m,2H), 2.03-1.86 (m, 2H), 1.72-1.61 (m, 1H) 147 N-(imidazo[1,2- ¹H NMR(500 MHz, methanol-d₄) δ 8.79 (s, (APCI(+)) a]pyridin-6- 1H), 8.21 (d, J= 2.1 Hz, 1H), 8.07 (s, 1H), m/e 470 ylmethyl)-2-{[(2R)- 8.02 (d, J =2.1 Hz, 1H), 8.00 (dd, J = 9.3, (M + H)⁺ tetrahydrofuran-2- 1.2 Hz, 1H),7.91 (d, J = 9.3 Hz, 1H), 4.66 ylmethyl](tetrahydro- (s, 2H), 4.61 (d, J= 12.8 Hz, 1H), 4.29- 2H-pyran-4- 4.19 (m, 2H), 4.06-3.96 (m, 2H), 3.85(dd, ylcarbonyl)amino}- J = 14.9, 6.9 Hz, 1H), 3.73 (dd, J = 13.9, 7.71,3-thiazole-5- Hz, 1H), 3.57-3.47 (m, 2H), 3.43 (ddd, J = carboxamide14.8, 8.4, 3.9 Hz, 1H), 2.11 (dt, J = 12.1, 5.4 Hz, 1H), 2.05-1.87 (m,3H), 1.83- 1.73 (m, 3H), 1.73-1.64 (m, 1H) 148 N-(imidazo[1,2- ¹H NMR(500 MHz, methanol-d₄) δ 8.78 (s, (APCI(+)) a]pyridin-6- 1H), 8.21 (d, J= 1.8 Hz, 1H), 8.06 (s, 1H), m/e 444 ylmethyl)-2-{(3- 8.02 (d, J = 2.2Hz, 1H), 8.00 (dd, J = 9.4, (M + H)⁺ methoxypropanoyl)[(2S)- 1.5 Hz,1H), 7.90 (d, J = 9.3 Hz, 1H), 4.66 tetrahydrofuran-2- (s, 2H), 4.52(dd, J = 14.9, 2.5 Hz, 1H), ylmethyl]amino}- 4.32-4.25 (m, 1H), 4.17(dd, J = 14.8, 8.9 1,3-thiazole-5- Hz, 1H), 3.92-3.83 (m, 1H), 3.81-3.74carboxamide (m, 2H), 3.71 (td, J = 7.7, 6.3 Hz, 1H), 3.36 (s, 3H),3.21-3.05 (m, 2H), 2.15-2.05 (m, 1H), 2.04-1.95 (m, 1H), 1.91 (ddt, J =7.5, 5.0, 1.9 Hz, 1H), 1.73-1.60 (m, 1H) 149 N-(imidazo[1,2- ¹H NMR (500MHz, methanol-d₄) δ 8.79 (s, (APCI(+)) a]pyridin-6- 1H), 8.21 (d, J =2.2 Hz, 1H), 8.08 (d, J = m/e 456 ylmethyl)-2- 0.7 Hz, 1H), 8.02 (d, J =2.1 Hz, 1H), 8.00 (M + H)⁺ {(tetrahydrofuran-3- (dd, J = 9.3, 1.3 Hz,1H), 7.91 (d, J = 9.3 ylcarbonyl)[(2S)- Hz, 1H), 4.66 (s, 2H), 4.61 (t,J = 13.2 Hz, tetrahydrofuran-2- 1H), 4.31-4.17 (m, 2H), 4.06 (ddd, J =ylmethyl]amino}- 14.8, 14.3, 7.3 Hz, 1H), 4.00-3.92 (m, 1,3-thiazole-5-2H), 3.90-3.79 (m, 3H), 3.71 (ddd, J = carboxamide 10.8, 8.3, 3.1 Hz,1H), 2.39-2.27 (m, 1H), 2.25-2.04 (m, 2H), 2.03-1.87 (m, 2H), 1.73-1.60(m, 1H) 150 N-(imidazo[1,2- ¹H NMR (500 MHz, methanol-d₄) δ 8.79 (s,(APCI(+)) a]pyridin-6- 1H), 8.21 (d, J = 1.9 Hz, 1H), 8.07 (d, J = m/e470 ylmethyl)-2-{[(2S)- 3.1 Hz, 1H), 8.02 (d, J = 2.2 Hz, 1H), 8.00 (M +H)⁺ tetrahydrofuran-2- (dd, J = 9.4, 1.5 Hz, 1H), 7.91 (d, J = 9.3ylmethyl](tetrahydro- Hz, 1H), 4.66 (s, 2H), 4.61 (d, J = 12.7 Hz,2H-pyran-4- 1H), 4.31-4.19 (m, 2H), 4.07-3.95 (m, ylcarbonyl)amino}-2H), 3.89-3.81 (m, 1H), 3.73 (td, J = 7.8, 1,3-thiazole-5- 6.1 Hz, 1H),3.58-3.47 (m, 2H), 3.47- carboxamide 3.39 (m, 1H), 2.16-2.05 (m, 1H),2.05- 1.86 (m, 3H), 1.77 (ddd, J = 14.6, 6.0, 2.5 Hz, 3H), 1.73-1.65 (m,1H) 183 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 480 ylmethyl)-2-{[(1-(M + H)⁺ methyl-1H-pyrazol-4- yl)acetyl](tetrahydro- furan-2-ylmethyl)amino}- 1,3-thiazole-5- carboxamide 184 2-{[(1,3-dimethyl-(ESI(+)) 1H-pyrazol-4- m/e 494 yl)acetyl](tetrahydro- (M + H)⁺ furan-2-ylmethyl)amino}-N- (imidazo[1,2- a]pyridin-6- ylmethyl)-1,3- thiazole-5-carboxamide 189 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 493ylmethyl)-2-{[3-(1- (M + H)⁺ methyl-1H-pyrrol-2- yl)propanoyl](tetra-hydrofuran-2- ylmethyl)amino}- 1,3-thiazole-5- carboxamide 1902-{[(1,5-dimethyl- (ESI(+)) 1H-pyrazol-3- m/e 494 yl)acetyl](tetrahydro-(M + H)⁺ furan-2- ylmethyl)amino}-N- (imidazo[1,2- a]pyridin-6-ylmethyl)-1,3- thiazole-5- carboxamide 191 N-(imidazo[1,2- (ESI(+))a]pyridin-6- m/e 483 ylmethyl)-2- (M + H)⁺ [(tetrahydrofuran-2-ylmethyl)(1,3- thiazol-4- ylacetyl)amino]-1,3- thiazole-5- carboxamide192 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ 8.73 (d, (APCI(+))a]pyridin-7- J = 7.0 Hz, 1H), 8.64 (d, J = 1.5 Hz, 1H), m/e 467ylmethyl)-2-{(1,2- 8.16 (d, J = 2.1 Hz, 1H), 8.12 (s, 1H), 7.98 (M + H)⁺oxazol-3- (d, J = 2.2 Hz, 1H), 7.80 (s, 1H), 7.46 (dd, J =ylacetyl)[(2R)- 7.0, 1.4 Hz, 1H), 6.52 (d, J = 1.6 Hz, 1H),tetrahydrofuran-2- 4.72 (s, 2H), 4.65 (dd, J = 14.9, 1.9 Hz,ylmethyl]amino}- 1H), 4.42 (d, J = 1.4 Hz, 2H), 4.32 (dd, J =1,3-thiazole-5- 11.6, 4.4 Hz, 1H), 4.23 (dd, J = 14.8, 9.0 carboxamideHz, 1H), 3.94 (dd, J = 14.9, 6.8 Hz, 1H), 3.76 (dd, J = 14.2, 7.7 Hz,1H), 2.21-2.07 (m, 1H), 2.08-1.87 (m, 2H), 1.69 (ddd, J = 15.8, 12.3,7.6 Hz, 1H) 193 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ 8.74 (d,(APCI(+)) a]pyridin-7- J = 7.0 Hz, 1H), 8.17 (d, J = 1.9 Hz, 1H), m/e481 ylmethyl)-2-{[(5- 8.11 (s, 1H), 7.99 (d, J = 2.1 Hz, 1H), 7.79 (M +H)⁺ methyl-1,2-oxazol- (s, 1H), 7.47 (d, J = 6.8 Hz, 1H), 6.16 (s,3-yl)acetyl][(2R)- 1H), 4.72 (s, 2H), 4.63 (d, J = 12.8 Hz, 1H),tetrahydrofuran-2- 4.36-4.27 (m, 3H), 4.21 (dd, J = 14.6, 9.4ylmethyl]amino}- Hz, 1H), 3.94 (dd, J = 15.1, 6.8 Hz, 1H),1,3-thiazole-5- 3.75 (dd, J = 14.3, 7.5 Hz, 1H), 2.43 (s, carboxamide3H), 2.13 (d, J = 8.1 Hz, 1H), 2.05-1.89 (m, 2H), 1.75-1.62 (m, 1H) 194N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ 8.74 (d, (APCI(+))a]pyridin-7- J = 7.0 Hz, 1H), 8.27 (d, J = 1.6 Hz, 1H), m/e 481ylmethyl)-2-{[3- 8.17 (d, J = 2.1 Hz, 1H), 8.10 (s, 1H), 7.99 (M + H)⁺(1,2-oxazol-5- (d, J = 2.1 Hz, 1H), 7.79 (s, 1H), 7.47 (d, J =yl)propanoyl][(2R)- 6.8 Hz, 1H), 6.23 (s, 1H), 4.72 (s, 2H),tetrahydrofuran-2- 4.55 (d, J = 12.6 Hz, 1H), 4.35-4.23 (m,ylmethyl]amino}- 1H), 4.15 (dd, J = 14.8, 9.0 Hz, 1H), 3.871,3-thiazole-5- (dd, J = 14.8, 6.9 Hz, 1H), 3.72 (dd, J = carboxamide14.0, 7.8 Hz, 1H), 3.46 (dd, J = 12.2, 6.1 Hz, 1H), 3.28-3.18 (m, 3H),2.10 (dd, J = 12.6, 7.2 Hz, 1H), 1.94 (dd, J = 15.7, 8.4 Hz, 2H),1.74-1.60 (m, 1H) 195 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ8.71 (d, (APCI(+)) a]pyridin-7- J = 7.0 Hz, 1H), 8.51 (s, 1H), 8.36 (s,1H), m/e 481 ylmethyl)-2-{[3- 8.11 (d, J = 17.0 Hz, 2H), 7.94 (d, J =2.0 (M + H)⁺ (1,2-oxazol-4- Hz, 1H), 7.76 (s, 1H), 7.42 (d, J = 6.8 Hz,yl)propanoyl][(2R)- 1H), 4.71 (s, 2H), 4.53 (d, J = 12.5 Hz, 1H),tetrahydrofuran-2- 4.27 (t, J = 6.7 Hz, 1H), 4.14 (dd, J = 14.9,ylmethyl]amino}- 9.1 Hz, 1H), 3.83 (dd, J = 14.9, 6.8 Hz, 1H),1,3-thiazole-5- 3.69 (dd, J = 13.8, 7.5 Hz, 1H), 3.26 (d, J =carboxamide 7.1 Hz, 1H), 3.09 (dd, J = 17.6, 6.4 Hz, 1H), 2.91 (dd, J =12.3, 6.4 Hz, 2H), 2.10 (dt, J = 12.3, 5.9 Hz, 1H), 2.03-1.84 (m, 2H),1.74- 1.58 (m, 1H) 196 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ9.00 (s, (APCI(+)) a]pyridin-7- 1H), 8.74 (d, J = 7.0 Hz, 1H), 8.17 (d,J = m/e 483 ylmethyl)-2-{[(2R)- 1.9 Hz, 1H), 8.11 (s, 1H), 7.98 (d, J =2.2 (M + H)⁺ tetrahydrofuran-2- Hz, 1H), 7.79 (s, 1H), 7.51 (s, 1H),7.47 (d, ylmethyl](1,3- J = 7.0 Hz, 1H), 4.72 (s, 2H), 4.63 (d, J =thiazol-4- 12.8 Hz, 1H), 4.49 (q, J = 16.9 Hz, 2H), ylacetyl)amino}-4.38-4.25 (m, 2H), 3.96 (dd, J = 14.9, 6.7 1,3-thiazole-5- Hz, 1H), 3.76(dd, J = 14.2, 7.6 Hz, 1H), carboxamide 2.19-2.08 (m, 1H), 2.06-1.98 (m,1H), 1.98-1.89 (m, 1H), 1.70 (td, J = 15.6, 7.6 Hz, 1H) 1972-{[(1,5-dimethyl- ¹H NMR (400 MHz, methanol-d₄) δ 8.74 (d, (APCI(+))1H-pyrazol-3- J = 7.0 Hz, 1H), 8.17 (d, J = 2.1 Hz, 1H), m/e 494yl)acetyl][(2R)- 8.10 (s, 1H), 7.99 (d, J = 2.1 Hz, 1H), 7.79 (M + H)⁺tetrahydrofuran-2- (s, 1H), 7.47 (d, J = 7.0 Hz, 1H), 6.01 (s,ylmethyl]amino}-N- 1H), 4.72 (s, 2H), 4.55 (d, J = 12.9 Hz, 1H),(imidazo[1,2- 4.30 (t, J = 7.9 Hz, 1H), 4.27-4.18 (m, a]pyridin-7- 2H),4.10 (t, J = 15.1 Hz, 1H), 3.94 (dd, J = ylmethyl)-1,3- 14.8, 6.8 Hz,1H), 3.82-3.68 (m, 4H), 2.27 thiazole-5- (s, 3H), 2.20-2.06 (m, 1H),2.00 (dd, J = carboxamide 13.5, 5.8 Hz, 1H), 1.97-1.87 (m, 1H), 1.76-1.58 (m, 1H) 198 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ 8.75(d, (APCI(+)) a]pyridin-7- J = 7.0 Hz, 1H), 8.17 (d, J = 2.1 Hz, 1H),m/e 494 ylmethyl)-2-{[3-(1- 8.09 (s, 1H), 7.99 (d, J = 2.1 Hz, 1H), 7.80(M + H)⁺ methyl-1H-pyrazol-4- (s, 1H), 7.47 (d, J = 8.2 Hz, 1H), 7.45(s, yl)propanoyl][(2R)- 1H), 7.36 (s, 1H), 4.72 (s, 2H), 4.50 (dd, J =tetrahydrofuran-2- 14.9, 2.3 Hz, 1H), 4.27 (t, J = 6.9 Hz, 1H),ylmethyl]amino}- 4.13 (dd, J = 14.9, 9.0 Hz, 1H), 3.89-3.761,3-thiazole-5- (m, 4H), 3.70 (dd, J = 14.1, 7.6 Hz, 1H), carboxamide3.21 (dt, J = 17.0, 7.2 Hz, 1H), 3.05 (dt, J = 16.9, 6.9 Hz, 1H), 2.88(t, J = 7.1 Hz, 2H), 2.09 (dt, J = 12.1, 7.6 Hz, 1H), 1.92 (ddd, J =19.6, 13.4, 7.1 Hz, 2H), 1.65 (dt, J = 19.6, 7.6 Hz, 1H) 1992-{[(3,5-dimethyl- ¹H NMR (400 MHz, methanol-d₄) δ 8.74 (d, (APCI(+))1,2-oxazol-4- J = 7.0 Hz, 1H), 8.17 (d, J = 2.0 Hz, 1H), m/e 495yl)acetyl][(2R)- 8.11 (s, 1H), 7.99 (d, J = 2.2 Hz, 1H), 7.79 (M + H)⁺tetrahydrofuran-2- (s, 1H), 7.47 (d, J = 7.1 Hz, 1H), 4.72 (s,ylmethyl]amino}-N- 2H), 4.68 (d, J = 13.1 Hz, 1H), 4.39-4.19(imidazo[1,2- (m, 3H), 4.03-3.88 (m, 2H), 3.77 (dd, J = a]pyridin-7-13.8, 7.6 Hz, 1H), 2.32 (s, 3H), 2.23-2.11 ylmethyl)-1,3- (m, 4H),2.09-1.91 (m, 2H), 1.77-1.63 thiazole-5- (m, 1H) carboxamide 202N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ 9.20 (s, (APCI(+))a]pyridin-7- 1H), 8.74 (d, J = 7.2 Hz, 1H), 8.17 (d, J = m/e 480ylmethyl)-2-{[(1- 2.0 Hz, 1H), 8.10 (s, 1H), 7.99 (d, J = 2.1 (M + H)⁺methyl-1H-pyrazol- Hz, 1H), 7.79 (s, 1H), 7.57 (s, 1H), 7.47 (d,4-yl)acetyl][(2R)- J = 5.9 Hz, 1H), 7.42 (s, 1H), 4.72 (s, 2H),tetrahydrofuran-2- 4.59 (d, J = 13.1 Hz, 1H), 4.31 (t, J = 7.1ylmethyl]amino}- Hz, 1H), 4.22 (dd, J = 14.7, 9.1 Hz, 1H),1,3-thiazole-5- 4.11 (s, 2H), 3.92 (dd, J = 14.9, 6.9 Hz, carboxamide1H), 3.87 (s, 3H), 3.76 (dd, J = 14.2, 7.7 Hz, 1H), 2.19-2.06 (m, 1H),2.00 (d, J = 7.3 Hz, 1H), 1.94 (dd, J = 13.4, 6.2 Hz, 1H), 1.69 (dt, J =15.5, 7.5 Hz, 1H) 203 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ8.74 (d, (APCI(+)) a]pyridin-7- J = 7.0 Hz, 1H), 8.17 (d, J = 2.0 Hz,1H), m/e 493 ylmethyl)-2-{[3-(1- 8.10 (s, 1H), 7.99 (d, J = 2.1 Hz, 1H),7.80 (M + H)⁺ methyl-1H-pyrrol-2- (s, 1H), 7.47 (d, J = 7.0 Hz, 1H),6.54 (d, J = yl)propanoyl][(2R)- 2.5 Hz, 1H), 5.91 (t, J = 3.1 Hz, 1H),5.83 tetrahydrofuran-2- (s, 1H), 4.72 (s, 2H), 4.50 (dd, J = 14.9, 2.3ylmethyl]amino}- Hz, 1H), 4.28 (t, J = 6.8 Hz, 1H), 4.12 (dd,1,3-thiazole-5- J = 14.8, 8.9 Hz, 1H), 3.85 (dd, J = 14.9, 6.8carboxamide Hz, 1H), 3.77-3.65 (m, 1H), 3.58 (s, 3H), 3.25 (t, J = 8.4Hz, 1H), 3.16-3.02 (m, 1H), 2.96 (t, J = 7.4 Hz, 2H), 2.10 (dt, J =12.0, 7.3 Hz, 1H), 2.04-1.81 (m, 2H), 1.66 (dt, J = 15.7, 7.4 Hz, 1H)

Example 58 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]butyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminobutyl)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide. ¹H NMR (500 MHz, DMSO-d₆, Temp=90° C.) δppm 8.79-8.76 (m, 1H), 8.10 (bs, 1H), 7.81-7.78 (m, 1H), 7.45-7.37 (m,2H), 7.02 (dd, J=9.5, 2.1 Hz, 1H), 6.04-5.96 (m, 1H), 3.93-3.85 (m, 2H),3.14-3.06 (m, 2H), 2.75-2.63 (m, 2H), 1.67-1.57 (m, 2H), 1.50-1.19 (m,16H), 1.07-0.91 (m, 2H); MS (ESI(+)) m/e 416 (M+H)⁺.

Example 594-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)benzamide

The title compound was prepared as described in Example 1, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for imidazo[1,2-a]pyridin-6-aminein Example 1C. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.87 (s, 1H), 8.46-8.41(m, 1H), 8.23-8.15 (m, 1H), 7.97-7.93 (m, 1H), 7.76-7.70 (m, 2H),7.57-7.51 (m, 2H), 7.49-7.43 (m, 2H), 7.21 (dd, J=9.2, 1.7 Hz, 1H), 6.77(t, J=5.9 Hz, 1H), 4.30 (d, J=5.8 Hz, 2H), 3.29-3.19 (m, 2H), 1.67-1.53(m, 1H), 1.45-1.35 (m, 2H), 0.93-0.87 (m, 6H); MS (ESI(+)) m/e 380(M+H)⁺.

Example 602-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide

The title compound was prepared as described in Example 3, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for imidazo[1,2-a]pyridin-6-aminein Example 3A. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ 9.34 (bs, 1H),8.71 (s, 1H), 8.38-8.33 (m, 1H), 8.23 (d, J=1.9 Hz, 1H), 7.97 (d, J=1.9Hz, 1H), 7.86-7.75 (m, 2H), 7.44-7.38 (m, 2H), 7.32-7.26 (m, 2H),6.69-6.62 (m, 1H), 4.43-4.38 (m, 2H), 2.29-2.18 (m, 3H), 1.81-1.68 (m,2H), 1.67-1.45 (m, 4H), 1.29-1.15 (m, 2H); MS (ESI(+)) m/e 392 (M+H)⁺.

Example 621-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)ureaExample 62A4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]butyl}piperidine

The title compound was prepared as described in Example 28A,substituting tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]butyl}piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 62B1-imidazo[1,2-a]pyridin-6-yl-3-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)urea

The title compound was prepared as described in Example 1A, substituting4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]butyl}piperidine for3-methylbutan-1-amine and 2-isopropoxyacetic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆/D₂O) δ ppm 9.18 (dd, J=1.9, 0.8 Hz, 1H),8.30-8.19 (m, 1H), 7.98 (d, J=2.1 Hz, 1H), 7.84 (d, J=9.7 Hz, 1H),7.76-7.72 (m, 1H), 4.03 (s, 4H), 3.72-3.52 (m, 1H), 3.14 (t, J=6.9 Hz,2H), 2.77 (s, 2H), 1.69 (dd, J=12.9, 2.3 Hz, 2H), 1.58-1.40 (m, 4H),1.41-1.31 (m, 2H), 1.31-1.21 (m, 2H), 1.11 (t, J=5.2 Hz, 6H), 1.03 (d,J=10.2 Hz, 2H); MS (ESI(+)) m/e 416 (M+H)⁺.

TABLE 5 The following Examples were prepared essentially as described inExample 62, substituting the appropriate carboxylic acid in Example 62B.Some products were purified by flash chromatography while others werepurified by reverse-phase HPLC. Accordingly, some Examples were isolatedas trifluoroacetic acid salts. Ex Name ¹H NMR MS 63 1-{4-[1-(1,4- ¹H NMR(400 MHz, DMSO-d₆/D₂O, (ESI(+)) dioxan-2- Temp = 90° C.) δ ppm 9.17 (dd,J = 2.0, 0.8 Hz, m/e 430 ylcarbonyl)piper- 1H), 8.23 (d, J = 1.7 Hz,1H), 7.97 (d, J = 2.1 (M + H)⁺ idin-4-yl]butyl}-3- Hz, 1H), 7.83 (d, J =9.7 Hz, 1H), 7.74 (dd, J = imidazo[1,2- 9.7, 1.9 Hz, 1H), 4.27 (dt, J =16.5, 8.3 Hz, a]pyridin-6-ylurea 1H), 3.80-3.70 (m, 2H), 3.70-3.58 (m,3H), 3.58-3.43 (m, 1H), 3.13 (q, J = 7.1 Hz, 2H), 1.69 (d, J = 11.6 Hz,2H), 1.56-1.43 (m, 4H), 1.42-1.21 (m, 6H), 1.03 (s, 2H) 64 1-{4-[1- ¹HNMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) (cyclopropylace- Temp = 90° C.) δppm 9.25-9.11 (m, 1H), 8.24 m/e 398 tyl)-piperidin-4- (d, J = 1.8 Hz,1H), 7.98 (d, J = 2.0 Hz, 1H), (M + H)⁺ yl]butyl}-3- 7.84 (d, J = 9.7Hz, 1H), 7.81-7.71 (m, 1H), imidazo[1,2- 3.98 (s, 1H), 3.24-3.06 (m,3H), 2.23 (d, J = a]pyridin-6-ylurea 6.7 Hz, 2H), 1.68 (d, J = 12.9 Hz,2H), 1.61- 1.41 (m, 4H), 1.39-1.20 (m, 4H), 1.09-0.85 (m, 4H), 0.49-0.35(m, 2H), 0.22-0.05 (m, 2H) 65 1-imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6-yl-3- Temp = 90° C.) δ ppm 9.24-9.11(m, 1H), 8.23 m/e 440 {4-[1-(4,4,4- (d, J = 2.1 Hz, 1H), 7.97 (d, J =2.0 Hz, 1H), (M + H)⁺ trifluorobutanoyl)pi- 7.83 (d, J = 9.7 Hz, 1H),7.77-7.69 (m, 1H), peridin-4- 3.14 (t, J = 6.9 Hz, 2H), 2.56 (dd, J =10.8, 4.4 yl]butyl}urea Hz, 3H), 2.51-2.40 (m, 2H), 1.69 (d, J = 12.0Hz, 2H), 1.63-1.43 (m, 4H), 1.41-1.22 (m, 4H), 0.98 (dd, J = 36.1, 8.5Hz, 2H) 66 1-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+))a]pyridin-6-yl-3- Temp = 90° C.) δ ppm 9.17 (dd, J = 1.9, 0.8 Hz, m/e402 {4-[1-(tetrahydro- 1H); 8.23 (d, J = 2.0 Hz, 1H), 7.97 (d, J = 2.1(M + H)⁺ 2H-pyran-4- Hz, 1H), 7.82 (d, J = 9.3 Hz, 1H), 7.73 (dd, J =ylacetyl)piperidin- 9.7, 1.9 Hz, 1H), 7.55 (dd, J = 8.4, 4.5 Hz, 2H),4-yl]butyl}urea 4.46 (d, J = 12.6 Hz, 2H), 3.16 (dd, J = 18.1, 11.2 Hz,2H), 2.78 (t, J = 12.3 Hz, 3H), 1.68 (d, J = 9.8 Hz, 2H), 1.54-1.42 (m,4H), 1.33 (s, 8H), 1.26 (t, J = 7.0 Hz, 3H), 1.11-0.99 (m, 2H) 671-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6-yl-3-Temp = 90° C.) δ ppm 9.17 (dd, J = 1.9, 0.8 Hz, m/e 442 {4-[1- 1H),8.30-8.19 (m, 1H), 7.98 (d, J = 2.1 Hz, (M + H)⁺ (tetrahydrofuran-2-1H), 7.83 (d, J = 9.6 Hz, 1H), 7.75 (dd, J = 9.6, ylacetyl)piperidin-1.9 Hz, 1H), 3.88-3.71 (m, 2H), 3.14 (t, J = 4-yl]butyl}urea 6.9 Hz,2H), 2.23 (t, J = 6.9 Hz, 2H), 1.91 (ttd, J = 10.7, 6.9, 3.5 Hz, 1H),1.68 (d, J = 12.1 Hz, 2H), 1.56 (t, J = 12.5 Hz, 2H), 1.53-1.42 (m, 4H),1.42-1.28 (m, 2H), 1.22 (m, 4H), 0.99 (d, J = 10.1 Hz, 2H) 68 1-{4-[1-¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) (cyclopentylcarbon- Temp = 90°C.) δ ppm 9.23-9.13 (m, 1H), 8.23 m/e 412 yl)piperidin-4- (d, J = 2.1Hz, 1H), 7.97 (d, J = 2.0 Hz, 1H), (M + H)⁺ yl]butyl}-3- 7.83 (d, J =9.7 Hz, 1H), 7.82-7.71 (m, 1H), imidazo[1,2- 4.12 (s, 2H), 3.98 (s, 1H),3.14 (t, J = 6.9 Hz, a]pyridin-6-ylurea 2H), 3.04-2.89 (m, 2H), 2.77 (s,2H), 1.87- 1.59 (m, 8H), 1.51-1.33 (m, 6H), 1.40-1.10 (m, 4H), 1.08-0.91(m, 2H) 69 1-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+))a]pyridin-6-yl-3- Temp = 90° C.) δ 9 ppm. 23-9.14 (m, 1H), 8.24 m/e 428{4-[1-(tetrahydro- (d, J = 1.9 Hz, 1H), 7.98 (d, J = 2.1 Hz, 1H), (M +H)⁺ 2H-pyran-4- 7.84 (d, J = 9.7 Hz, 1H), 7.79-7.68 (m, 1H),ylcarbonyl)piperi- 4.11 (s, 2H), 3.88-3.77 (m, 2H), 3.51-3.36din-4-yl]butyl}urea (m, 2H), 3.21-3.09 (m, 2H), 2.92-2.73 (m, 2H),1.76-1.56 (m, 4H), 1.56-1.42 (m, 6H), 1.45-1.18 (m, 4H), 1.04-0.87 (m,2H) 70 1-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+))a]pyridin-6-yl-3- Temp = 90° C.) δ ppm 9.17 (dd, J = 1.9, 0.8 Hz, m/e432 (4-{1-[(2- 1H), 8.24 (d, J = 1.9 Hz, 1H), 7.98 (d, J = 2.1 (M + H)⁺methoxyethoxy)ace- Hz, 1H), 7.84 (d, J = 9.7 Hz, 1H), 7.75 (dd, J =tyl]piperidin-4- 9.7, 1.9 Hz, 1H), 4.09 (d, J = 7.6 Hz, 2H), 3.56yl}butyl)urea (dd, J = 6.0, 3.8 Hz, 2H), 3.47 (dd, J = 5.7, 3.7 Hz, 2H),3.26 (s, 2H), 3.19-3.07 (m, 2H), 1.68 (dd, J = 13.0, 2.2 Hz, 2H), 1.48(dt, J = 14.1, 7.0 Hz, 4H), 1.40-1.22 (m, 6H), 1.04 (d, J = 9.3 Hz, 2H)71 1-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+))a]pyridin-6-yl-3- Temp = 90° C.) δ ppm 9.26-9.11 (m, 1H), 8.23 m/e 443{4-[1-(morpholin-4- (d, J = 1.8 Hz, 1H), 7.98 (d, J = 2.1 Hz, 1H), (M +H)⁺ ylacetyl)piperidin- 7.83 (t, J = 8.1 Hz, 1H), 7.80-7.71 (m, 1H),4-yl]butyl}urea 4.22 (s, 2H), 3.98 (s, 1H), 3.93-3.84 (m, 4H), 3.62 (s,1H), 3.18-3.07 (m, 2H), 2.71 (s, 2H), 1.80-1.67 (m, 2H), 1.51 (dq, J =21.7, 7.0 Hz, 4H), 1.42-1.20 (m, 6H), 1.07 (s, 2H) 72 1-imidazo[1,2- ¹HNMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6-yl-3- Temp = 90° C.) δppm 9.25-9.14 (m, 1H), 8.24 m/e 414 {4-[1- (d, J = 1.9 Hz, 1H), 7.98 (d,J = 2.0 Hz, 1H), (M + H)⁺ (tetrahydrofuran-3- 7.84 (d, J = 9.7 Hz, 1H),7.79-7.69 (m, 1H), ylcarbonyl)piperi- 3.85 (t, J = 8.1 Hz, 2H), 3.70 (h,J = 7.8 Hz, din-4-yl]butyl}urea 4H), 3.20-3.08 (m, 2H), 2.09-1.91 (m,2H), 1.70 (d, J = 12.1 Hz, 2H), 1.61-1.43 (m, 4H), 1.37-1.24 (m, 4H),1.08-0.88 (m, 2H) 73 1-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O,(ESI(+)) a]pyridin-6-yl-3- Temp = 90° C.) δ ppm 9.22-9.12 (m, 1H), 8.24m/e 428 {4-[1- (d, J = 2.1 Hz, 1H), 7.98 (d, J = 2.0 Hz, 1H), (M + H)⁺(tetrahydrofuran-3- 7.84 (d, J = 9.7 Hz, 1H), 7.79-7.69 (m, 1H),ylacetyl)piperidin- 3.98 (s, 1H), 3.86-3.76 (m, 1H), 3.75-3.684-yl]butyl}urea (m, 1H), 3.68-3.57 (m, 1H), 3.28-3.23 (m, 1H), 3.14 (t,J = 6.9 Hz, 2H), 2.50-2.43 (m, 1H), 2.43-2.30 (m, 2H), 2.09-1.92 (m,1H), 1.68 (d, J = 13.3 Hz, 2H), 1.56-1.41 (m, 6H), 1.38-1.29 (m, 2H),1.25 (dd, J = 14.2, 6.0 Hz, 2H), 1.00 (d, J = 10.2 Hz, 2H) 741-imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) a]pyridin-6-yl-3-Temp = 90° C.) δ ppm 9.18 (d, J = 1.1 Hz, 1H), m/e 414 {4-[1- 8.24 (d, J= 2.0 Hz, 1H), 7.98 (d, J = 2.0 Hz, (M + H)⁺ (tetrahydrofuran-2- 1H),7.84 (d, J = 9.6 Hz, 1H), 7.79-7.65 (m, ylcarbonyl)piperi- 1H), 4.59 (t,J = 6.7 Hz, 1H), 4.12 (s, 2H), 3.88- din-4-yl]butyl}urea 3.62 (m, 2H),3.16 (dd, J = 18.1, 11.3 Hz, 2H), 2.02-1.93 (m, 2H), 1.93-1.72 (m, 2H),1.69 (d, J = 12.7 Hz, 2H), 1.58-1.43 (m, 4H), 1.42-1.19 (m, 5H),1.17-0.87 (m, 2H) 107 1-[4-(1- ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.82-(ESI(+)) benzoylpiperidin- 8.77 (m, 1H), 7.76 (s, 1H), 7.50 (s, 1H),7.48- m/e 420 4-yl)butyl]-3- 7.40 (m, 4H), 7.42-7.33 (m, 2H), 7.09 (dd,J = (M + H)⁺ imidazo[1,2- 9.5, 2.0 Hz, 1H), 4.65-4.57 (m, 1H), 3.74-a]pyridin-6-ylurea 3.65 (m, 1H), 3.21 (t, J = 6.9 Hz, 2H), 3.13- 3.03(m, 1H), 2.88-2.78 (m, 1H), 1.90-1.82 (m, 1H), 1.74-1.46 (m, 4H),1.48-1.26 (m, 4H), 1.28-1.04 (m, 2H) 270 1-[4-(1- (ESI(+))benzoylpiperidin- m/e 420 4-yl)butyl]-3- (M + H)⁺ imidazo[1,2-a]pyridin-7-ylurea

Example 75N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamideExample 75A5-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and5-bromothiophene-2-carboxylic acid for 4-nitrobenzoic acid.

Example 75BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting5-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiophene-2-carboxamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.99 (t, J=5.8 Hz, 1H),8.46 (s, 1H), 8.14 (s, 1H), 7.95 (s, 1H), 7.79 (s, 1H), 7.69 (d, J=3.9Hz, 1H), 7.49-7.58 (m, 2H), 7.20 (d, J=4.0 Hz, 2H), 4.43 (d, J=5.7 Hz,2H), 3.91 (d, J=7.2 Hz, 2H), 2.11 (dq, J=13.6, 6.8 Hz, 1H), 0.84 (d,J=6.7 Hz, 6H); MS (ESI(+)) m/e 380 (M+H)⁺.

TABLE 6 The following Examples were prepared essentially as described inExample 75, substituting the appropriate carboxylic acid and amine inExample 75A and the appropriate boronate in Example 75B. Some boronateswere Boc-protected and required deprotection as in Example 28A. Ex Name¹H NMR MS 120 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.87(ESI(+)) a]pyridin-6- (t, J = 6.0 Hz, 1 H), 8.46 (s, 1 H), 8.14 (s, 1H), m/e 364 ylmethyl)-5-[1-(2- 7.96 (s, 1 H), 7.87 (s, 1 H), 7.53 (d, J= 6.8 Hz, (M + H)⁺ methylpropyl)-1H- 2 H), 7.21 (dd, J = 9.3, 1.4 Hz, 1H), 7.14 (d, pyrazol-4-yl]furan- J = 3.6 Hz, 1 H), 6.64 (d, J = 3.5 Hz,1 H), 4.44 2-carboxamide (d, J = 6.0 Hz, 2 H), 3.94 (d, J = 7.2 Hz, 2H), 2.11 (dq, J = 13.6, 6.8 Hz, 1 H), 0.83 (d, J = 6.7 Hz, 6 H) 174N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.04 (ESI(+))a]pyridin-7- (t, J = 6.0 Hz, 1 H), 8.48 (d, J = 7.0 Hz, 1 H), m/e 380ylmethyl)-5-[1-(2- 8.14 (s, 1 H), 7.88 (s, 1 H), 7.80 (s, 1 H), 7.73(M + H)⁺ methylpropyl)-1H- (d, J = 3.8 Hz, 1 H), 7.51 (s, 1 H), 7.38 (s,1 H), pyrazol-4- 7.21 (d, J = 3.9 Hz, 1 H), 6.84 (dd, J = 7.0, 1.5yl]thiophene-2- Hz, 1 H), 4.46 (d, J = 5.9 Hz, 2 H), 3.91 (d,carboxamide J = 7.3 Hz, 2 H), 2.11 (dq, J = 13.6, 6.7, 6.6 Hz, 1 H),0.84 (d, J = 6.7 Hz, 6 H) 175 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆)δ ppm 9.09 a]pyridin-6- (t, J = 5.9 Hz, 1 H), 8.81 (s, 1 H), 8.47 (s, 1H), ylmethyl)-5-[1-(2- 8.31 (s, 1 H), 7.95 (s, 1 H), 7.76 (d, J = 3.9Hz, methylpropanoyl)- 1 H), 7.54 (t, J = 4.6 Hz, 2 H), 7.50 (d, J = 3.91H-pyrazol-4- Hz, 1 H), 7.20 (dd, J = 9.2, 1.5 Hz, 1 H), 4.44yl]thiophene-2- (d, J = 5.9 Hz, 2 H), 3.77 (dq, J = 6.9 Hz, 1 H),carboxamide 1.21 (d, J = 6.9 Hz, 6 H) 176 5-[1-(2-hydroxy-2- ¹H NMR (400MHz, DMSO-d₆) δ ppm 9.00 (ESI(+)) methylpropyl)-1H- (t, J = 5.9 Hz, 1H), 8.46 (s, 1 H), 8.03 (s, 1 H), m/e 396 pyrazol-4-yl]-N- 7.95 (s, 1H), 7.78 (s, 1 H), 7.69 (d, J = 3.8 Hz, (M + H)⁺ (imidazo[1,2- 1 H),7.49-7.58 (m, 2 H), 7.16-7.25 (m, 2 a]pyridin-6- H), 4.76 (s, 1 H), 4.42(d, J = 5.7 Hz, 2 H), 4.01 ylmethyl)thiophene- (s, 2 H), 1.06 (s, 6 H)2-carboxamide 177 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00a]pyridin-6- (t, J = 5.9 Hz, 1 H), 8.46 (s, 1 H), 8.19 (s, 1 H),ylmethyl)-5-{1-[(3- 7.95 (s, 1 H), 7.83 (s, 1 H), 7.70 (d, J = 3.9 Hz,methyloxetan-3- 1 H), 7.48-7.58 (m, 2 H), 7.15-7.24 (m, 2 yl)methyl]-1H-H), 4.59 (d, J = 6.0 Hz, 2 H), 4.42 (d, J = 5.9 Hz, pyrazol-4- 2 H),4.33 (s, 2 H), 4.22 (d, J = 6.0 Hz, 2 H), yl}thiophene-2- 1.13 (s, 3 H)carboxamide 178 5-[1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.99(cyclobutylmethyl)- (t, J = 5.9 Hz, 1 H), 8.46 (s, 1 H), 8.13 (s, 1 H),1H-pyrazol-4-yl]- 7.95 (s, 1 H), 7.77 (s, 1 H), 7.69 (d, J = 3.9 Hz,N-(imidazo[1,2- 1 H), 7.48-7.57 (m, 2 H), 7.16-7.23 (m, 2 a]pyridin-6-H), 4.42 (d, J = 5.7 Hz, 2 H), 4.12 (d, J = 7.3 Hz, ylmethyl)thiophene-2 H), 2.74 (dq, J = 7.5, 7.4 Hz, 1 H), 1.90-2.02 2-carboxamide (m, 2 H),1.67-1.90 (m, 4 H) 179 5-[1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.99(ESI(+)) (cyclohexylmethyl)- (t, J = 5.9 Hz, 1 H), 8.46 (s, 1 H), 8.12(s, 1 H), m/e 420 1H-pyrazol-4-yl]- 7.95 (s, 1 H), 7.78 (s, 1 H), 7.69(d, J = 3.9 Hz, (M + H)⁺ N-(imidazo[1,2- 1 H), 7.48-7.57 (m, 2 H),7.14-7.26 (m, 2 a]pyridin-6- H), 4.42 (d, J = 5.9 Hz, 2 H), 3.93 (d, J =7.2 Hz, ylmethyl)thiophene- 2 H), 1.72-1.88 (m, 1 H), 1.54-1.70 (m, 32-carboxamide H), 1.50 (d, J = 12.1 Hz, 2 H), 1.03-1.28 (m, 3 H),0.85-1.01 (m, 2 H) 180 5-{1-[(2R)-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm8.99 hydroxybutyl]-1H- (t, J = 5.8 Hz, 1 H), 8.46 (s, 1 H), 8.08 (s, 1H), pyrazol-4-yl}-N- 7.95 (s, 1 H), 7.78 (s, 1 H), 7.69 (d, J = 3.9 Hz,(imidazo[1,2- 1 H), 7.50-7.58 (m, 2 H), 7.17-7.23 (m, 2 a]pyridin-6- H),4.92 (d, J = 5.4 Hz, 1 H), 4.42 (d, J = 5.7 Hz, ylmethyl)thiophene- 2H), 4.03-4.12 (m, 1 H), 3.93-4.02 (m, 1 2-carboxamide H), 3.66-3.76 (m,1 H), 1.20-1.44 (m, 2 H), 0.88 (t, J = 7.4 Hz, 3 H) 1825-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.04methylpropyl)-1H- (t, J = 5.9 Hz, 1 H), 8.48 (d, J = 7.0 Hz, 1 H),pyrazol-4-yl]-N- 8.04 (s, 1 H), 7.88 (s, 1 H), 7.79 (s, 1 H), 7.73(imidazo[1,2- (d, J = 3.8 Hz, 1 H), 7.51 (s, 1 H), 7.38 (s, 1 H),a]pyridin-7- 7.23 (d, J = 3.8 Hz, 1 H), 6.84 (dd, J = 7.0, 1.3ylmethyl)thiophene- Hz, 1 H), 4.75 (s, 1 H), 4.46 (d, J = 5.9 Hz, 22-carboxamide H), 4.01 (s, 2 H), 1.07 (s, 6 H) 186 N-(imidazo[1,2- ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.00 (ESI(+)) a]pyridin-6- (t, J = 5.8 Hz,1 H), 8.46 (s, 1 H), 8.07 (s, 1 H), m/e 422 ylmethyl)-5-[1- 7.95 (s, 1H), 7.78 (s, 1 H), 7.69 (d, J = 3.8 Hz, (M + H)⁺ (tetrahydro-2H- 1 H),7.48-7.57 (m, 2 H), 7.14-7.27 (m, 2 pyran-2-ylmethyl)- H), 4.42 (d, J =5.9 Hz, 2 H), 4.05-4.15 (m, 2 1H-pyrazol-4- H), 3.83 (d, J = 11.1 Hz, 1H), 3.55-3.71 (m, 1 yl]thiophene-2- H), 3.19-3.37 (m, 2 H), 1.68-1.85(m, 1 H), carboxamide 1.48-1.63 (m, 1 H), 1.32-1.50 (m, 2 H), 1.06-1.29(m, 1 H) 200 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00a]pyridin-6- (t, J = 5.8 Hz, 1 H), 8.46 (s, 1 H), 8.20 (s, 1 H),ylmethyl)-5-[1- 7.95 (s, 1 H), 7.81 (s, 1 H), 7.69 (d, J = 3.9 Hz,(tetrahydrofuran-3- 1 H), 7.49-7.57 (m, 2 H), 7.15-7.24 (m, 2ylmethyl)-1H- H), 4.42 (d, J = 5.7 Hz, 2 H), 4.10 (d, J = 7.5 Hz,pyrazol-4- 2 H), 3.69-3.79 (m, 1 H), 3.56-3.70 (m, 2 yl]thiophene-2- H),3.46 (dd, J = 8.7, 5.4 Hz, 2 H), 1.81-1.98 carboxamide (m, 1 H),1.52-1.65 (m, 1 H) 201 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm8.99 a]pyridin-6- (t, J = 5.8 Hz, 1 H), 8.46 (s, 1 H), 8.14 (s, 1 H),ylmethyl)-5-[1- 7.95 (s, 1 H), 7.80 (s, 1 H), 7.69 (d, J = 3.9 Hz,(tetrahydro-2H- 1 H), 7.48-7.58 (m, 2 H), 7.12-7.25 (m, 2pyran-4-ylmethyl)- H), 4.43 (d, J = 5.7 Hz, 2 H), 4.00 (d, J = 7.2 Hz,1H-pyrazol-4- 2 H), 3.81 (dd, J = 11.3, 2.9 Hz, 2 H), 3.24 (td,yl]thiophene-2- J = 11.6, 1.7 Hz, 2 H), 1.91-2.18 (m, 1 H), carboxamide1.39 (dd, J = 12.7, 1.4 Hz, 2 H), 1.14-1.30 (m, 2 H) 206 N-(imidazo[1,2-¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.99 a]pyridin-6- (t, J = 5.8 Hz, 1 H),8.46 (s, 1 H), 8.15 (s, 1 H), ylmethyl)-5-[1- 7.95 (s, 1 H), 7.80 (s, 1H), 7.69 (d, J = 3.9 Hz, (tetrahydro-2H- 1 H), 7.53 (t, J = 4.6 Hz, 2H), 7.15-7.26 (m, 2 pyran-3-ylmethyl)- H), 4.43 (d, J = 5.9 Hz, 2 H),4.02 (dd, J = 7.2, 1H-pyrazol-4- 3.2 Hz, 2 H), 3.64-3.72 (m, 1 H), 3.61(dd, yl]thiophene-2- J = 11.1, 3.3 Hz, 1 H), 3.15 (dd, J = 11.2, 8.8 Hz,carboxamide 1 H), 1.96-2.18 (m, 1 H), 1.52-1.70 (m, 2 H), 1.34-1.51 (m,1 H), 1.10-1.31 (m, 2 H) 219 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δppm 8.99 a]pyridin-6- (t, J = 5.9 Hz, 1 H), 8.46 (s, 1 H), 8.10 (s, 1H), ylmethyl)-5-[1- 7.95 (s, 1 H), 7.79 (s, 1 H), 7.70 (d, J = 3.9 Hz,(tetrahydrofuran-2- 1 H), 7.46-7.60 (m, 2 H), 7.11-7.26 (m, 2ylmethyl)-1H- H), 4.43 (d, J = 5.9 Hz, 2 H), 4.04-4.25 (m, 3 pyrazol-4-H), 3.69-3.80 (m, 1 H), 3.62 (q, J = 7.4 Hz, 1 yl]thiophene-2- H),1.86-2.01 (m, 1 H), 1.68-1.84 (m, 2 H), carboxamide 1.52-1.67 (m, 1 H)247 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 422 ylmethyl)-5-[1- (M +H)⁺ (tetrahydro-2H- pyran-2-ylmethyl)- 1H-pyrazol-4- yl]thiophene-2-carboxamide 248 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 408ylmethyl)-5-[1- (M + H)⁺ (tetrahydrofuran-2- ylmethyl)-1H- pyrazol-4-yl]thiophene-2- carboxamide 252 N-(imidazo[1,2- (ESI(+)) a]pyridin-7-m/e 408 ylmethyl)-5-[1- (M + H)⁺ (tetrahydrofuran-3- ylmethyl)-1H-pyrazol-4- yl]thiophene-2- carboxamide 253 N-(imidazo[1,2- ¹H NMR (300MHz, DMSO-d₆) δ ppm 9.04 (ESI(+)) a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.49(dd, J = 7.2, 1.1 Hz, m/e 422 ylmethyl)-5-[1- 1H), 8.16 (s, 1H), 7.89(t, J = 1.0 Hz, 1H), (M + H)⁺ (tetrahydro-2H- 7.82 (s, 1H), 7.74 (d, J =3.9 Hz, 1H), 7.52 (d, pyran-3-ylmethyl)- J = 1.4 Hz, 1H), 7.40 (s, 1H),7.22 (d, J = 3.8 1H-pyrazol-4- Hz, 1H), 6.85 (dd, J = 7.0, 1.7 Hz, 1H),4.48 yl]thiophene-2- (d, J = 5.7 Hz, 2H), 4.03 (dd, J = 7.3, 2.1 Hz,carboxamide 2H), 3.76-3.57 (m, 2H), 3.42-3.32 (m, 1H), 3.17 (dd, J =11.2, 8.7 Hz, 1H), 2.15-1.98 (m, 1H), 1.77-1.54 (m, 2H), 1.54-1.35 (m,1H), 1.32-1.14 (m, 1H) 254 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 408ylmethyl)-5-{1-[(3- (M + H)⁺ methyloxetan-3- yl)methyl]-1H- pyrazol-4-yl}thiophene-2- carboxamide 265 N-(imidazo[1,2- (ESI(+)) a]pyridin-7-m/e 422 ylmethyl)-5-[1- (M + H)⁺ (tetrahydro-2H- pyran-4-ylmethyl)-1H-pyrazol-4- yl]thiophene-2- carboxamide 269 N-(imidazo[1,2- ¹H NMR(300 MHz, DMSO-d₆) δ ppm 9.03 (ESI(+)) a]pyridin-7- (t, J = 5.9 Hz, 1H),8.53-8.45 (m, 1H), 8.13 m/e 382 ylmethyl)-5-[1-(2- (s, 1H), 7.89 (s,1H), 7.81 (s, 1H), 7.74 (d, J = (M + H)⁺ methoxyethyl)-1H- 3.9 Hz, 1H),7.52 (d, J = 1.1 Hz, 1H), 7.40 (s, pyrazol-4- 1H), 7.22 (d, J = 3.8 Hz,1H), 6.85 (dd, J = yl]thiophene-2- 7.0, 1.6 Hz, 1H), 4.48 (d, J = 5.9Hz, 2H), carboxamide 4.27 (t, J = 5.3 Hz, 2H), 3.70 (t, J = 5.3 Hz, 2H),3.24 (s, 3H) 272 5-[1- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04 (ESI(+))(cyclohexylmethyl)- (t, J = 6.1 Hz, 1H), 8.49 (d, J = 7.8 Hz, 1H), m/e448 5-ethyl-1H- 7.89 (s, 1H), 7.78 (d, J = 4.1 Hz, 1H), 7.72 (s, (M +H)⁺ pyrazol-4-yl]-N- 1H), 7.52 (d, J = 1.0 Hz, 1H), 7.40 (s, 1H),(imidazo[1,2- 7.17 (d, J = 4.1 Hz, 1H), 6.85 (dd, J = 7.1, 1.7a]pyridin-7- Hz, 1H), 4.48 (d, J = 5.8 Hz, 2H), 3.90 (d, J =ylmethyl)thiophene- 7.5 Hz, 2H), 2.87 (q, J = 7.2 Hz, 2H), 1.79-2-carboxamide 1.95 (m, 1H), 1.59-1.73 (m, J = 3.4 Hz, 3H), 1.54 (d, J =12.5 Hz, 2H), 1.09-1.25 (m, 6H), 0.93-1.08 (m, J = 11.9 Hz, 2H) 273N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (ESI(+))a]pyridin-7- (t, J = 5.9 Hz, 1H), 8.49 (d, J = 7.1 Hz, 1H), m/e 492ylmethyl)-5-{1-[(1- 7.89 (s, 1H), 7.79 (d, J = 3.7 Hz, 1H), 7.74 (s,(M + H)⁺ methoxy-3,3- 1H), 7.52 (d, J = 1.0 Hz, 1H), 7.40 (s, 1H),dimethylcyclohex- 7.18 (d, J = 4.1 Hz, 1H), 6.85 (dd, J = 7.1, 1.7yl)methyl]-5-methyl- Hz, 1H), 4.48 (d, J = 5.8 Hz, 2H), 3.97-4.161H-pyrazol-4- (m, 2H), 3.20 (s, 3H), 2.45 (s, 3H), 1.64-1.78yl}thiophene-2- (m, 1H), 1.27-1.59 (m, 4H), 0.99-1.24 (m, carboxamide3H), 0.96 (s, 3H), 0.85 (s, 3H) 293 N-(imidazo[1,2- ¹H NMR (300 MHz,DMSO-d₆) δ ppm 9.03 (ESI(+)) a]pyridin-7- (s, 1H), 8.47 (t, J = 9.6 Hz,1H), 8.17 (s, 1H), m/e 366 ylmethyl)-5-(1- 7.89 (s, 1H), 7.80 (s, 1H),7.74 (d, J = 3.9 Hz, (M + H)⁺ propyl-1H-pyrazol- 1H), 7.52 (d, J = 1.1Hz, 1H), 7.40 (s, 1H), 4-yl)thiophene-2- 7.22 (d, J = 3.8 Hz, 1H), 6.83(dt, J = 14.9, 7.4 carboxamide Hz, 1H), 4.48 (d, J = 5.9 Hz, 2H), 4.07(t, J = 7.0 Hz, 2H), 1.81 (dd, J = 14.4, 7.2 Hz, 2H), 0.84 (t, J = 7.4Hz, 3H) 294 N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03(ESI(+)) a]pyridin-7- (t, J = 5.9 Hz, 1H), 8.49 (d, J = 7.0 Hz, 1H), m/e437 ylmethyl)-5-{1-[2- 8.17 (s, 1H), 7.89 (s, 1H), 7.80 (s, 1H), 7.74(M + H)⁺ (morpholin-4- (d, J = 3.9 Hz, 1H), 7.52 (d, J = 1.2 Hz, 1H),yl)ethyl]-1H- 7.40 (s, 1H), 7.22 (d, J = 3.8 Hz, 1H), 6.85 pyrazol-4-(dd, J = 7.0, 1.5 Hz, 1H), 4.48 (d, J = 5.9 Hz, yl}thiophene-2- 2H),4.24 (t, J = 6.5 Hz, 2H), 3.59-3.49 (m, carboxamide 4H), 2.72 (t, J =6.5 Hz, 2H), 2.45-2.35 (m, 4H) 295 5-(1-ethyl-1H- ¹H NMR (300 MHz,DMSO-d₆) δ ppm 9.02 (ESI(+)) pyrazol-4-yl)-N- (t, J = 5.9 Hz, 1H), 8.49(d, J = 7.0 Hz, 1H), m/e 352 (imidazo[1,2- 8.17 (s, 1H), 7.89 (s, 1H),7.79 (s, 1H), 7.74 (M + H)⁺ a]pyridin-7- (d, J = 3.8 Hz, 1H), 7.52 (d, J= 1.2 Hz, 1H), ylmethyl)thiophene- 7.40 (s, 1H), 7.21 (d, J = 3.8 Hz,1H), 6.85 2-carboxamide (dd, J = 7.0, 1.6 Hz, 1H), 4.48 (d, J = 5.9 Hz,2H), 4.15 (q, J = 7.3 Hz, 2H), 1.39 (t, J = 7.3 Hz, 3H) 296 5-[1-(1,1-¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.05 (ESI(+)) dioxidotetrahydro- (t, J =6.0 Hz, 1H), 8.49 (d, J = 6.9 Hz, 1H), m/e 442 thiophen-3-yl)-1H- 8.32(s, 1H), 7.94 (s, 1H), 7.89 (s, 1H), 7.76 (M + H)⁺ pyrazol-4-yl]-N- (d,J = 3.8 Hz, 1H), 7.52 (d, J = 1.1 Hz, 1H), (imidazo[1,2- 7.40 (s, 1H),7.26 (d, J = 3.8 Hz, 1H), 6.85 a]pyridin-7- (dd, J = 7.0, 1.6 Hz, 1H),5.35-5.18 (m, 1H), ylmethyl)thiophene- 4.48 (d, J = 5.9 Hz, 2H), 3.75(dd, J = 13.6, 2-carboxamide 8.2 Hz, 1H), 3.48 (m, 2H), 3.35-3.20 (m,1H), 2.78-2.53 (m, 2H) 300 N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δppm 9.04 (ESI(+)) a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 7.0,0.8 Hz, m/e 430 ylmethyl)-5-{1-[2- 1H), 8.25 (s, 1H), 7.89 (d, J = 1.4Hz, 2H), (M + H)⁺ (methylsulfonyl)eth- 7.75 (d, J = 3.9 Hz, 1H), 7.52(d, J = 1.2 Hz, yl]-1H-pyrazol-4- 1H), 7.40 (s, 1H), 7.24 (d, J = 3.8Hz, 1H), yl}thiophene-2- 6.85 (dd, J = 7.0, 1.7 Hz, 1H), 4.57 (t, J =6.9 carboxamide Hz, 2H), 4.48 (d, J = 5.9 Hz, 2H), 3.73 (t, J = 6.9 Hz,2H), 2.93 (s, 3H) 304 5-{1-[(2R)-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.02(ESI(+)) hydroxypropyl]- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 7.0, 0.7 Hz,m/e 382 1H-pyrazol-4-yl}- 1H), 8.09 (s, 1H), 7.89 (s, 1H), 7.80 (d, J =0.5 (M + H)⁺ N-(imidazo[1,2- Hz, 1H), 7.74 (d, J = 3.9 Hz, 1H), 7.52 (d,J = a]pyridin-7- 1.2 Hz, 1H), 7.40 (s, 1H), 7.22 (d, J = 3.8 Hz,ylmethyl)thiophene- 1H), 6.85 (dd, J = 7.0, 1.6 Hz, 1H), 4.93 (d, J =2-carboxamide 4.7 Hz, 1H), 4.48 (d, J = 5.9 Hz, 2H), 4.11- 3.93 (m, 3H),1.12-0.98 (m, 3H) 316 5-[1-(1,4-dioxan-2- ¹H NMR (300 MHz, DMSO-d₆) δppm 9.03 (ESI(+)) ylmethyl)-1H- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 7.0,0.7 Hz, m/e 424 pyrazol-4-yl]-N- 1H), 8.12 (s, 1H), 7.89 (s, 1H), 7.82(s, 1H), (M + H)⁺ (imidazo[1,2- 7.74 (d, J = 3.8 Hz, 1H), 7.52 (d, J =1.2 Hz, a]pyridin-7- 1H), 7.40 (s, 1H), 7.23 (d, J = 3.8 Hz, 1H),ylmethyl)thiophene- 6.85 (dd, J = 7.0, 1.6 Hz, 1H), 4.48 (d, J = 5.92-carboxamide Hz, 2H), 4.20-4.14 (m, 2H), 3.96-3.83 (m, 1H), 3.79-3.70(m, 2H), 3.68-3.39 (m, 3H), 3.29-3.21 (m, 1H) 317 5-[1-(2- ¹H NMR (300MHz, DMSO-d₆) δ ppm 9.02 (ESI(+)) hydroxyethyl)-1H- (t, J = 5.9 Hz, 1H),8.49 (dd, J = 7.0, 0.7 Hz, m/e 368 pyrazol-4-yl]-N- 1H), 8.12 (s, 1H),7.89 (d, J = 0.8 Hz, 1H), (M + H)⁺ (imidazo[1,2- 7.80 (d, J = 0.6 Hz,1H), 7.74 (d, J = 3.8 Hz, a]pyridin-7- 1H), 7.52 (d, J = 1.2 Hz, 1H),7.40 (s, 1H), ylmethyl)thiophene- 7.22 (d, J = 3.9 Hz, 1H), 6.85 (dd, J= 7.0, 1.6 2-carboxamide Hz, 1H), 4.92 (t, J = 5.3 Hz, 1H), 4.48 (d, J =5.9 Hz, 2H), 4.15 (t, J = 5.6 Hz, 2H), 3.75 (q, J = 5.5 Hz, 2H) 3445-{1-[(1,1- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04 (ESI(+))dioxidotetrahydro- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 7.0, 0.8 Hz, m/e470 2H-thiopyran-3- 1H), 8.19 (d, J = 0.4 Hz, 1H), 7.89 (d, J = 0.8 (M +H)⁺ yl)methyl]-1H- Hz, 1H), 7.86 (d, J = 0.5 Hz, 1H), 7.75 (d, J =pyrazol-4-yl}-N- 3.9 Hz, 1H), 7.52 (d, J = 1.2 Hz, 1H), 7.40 (s,(imidazo[1,2- 1H), 7.24 (d, J = 3.9 Hz, 1H), 6.85 (dd, J = a]pyridin-7-7.0, 1.7 Hz, 1H), 4.48 (d, J = 5.8 Hz, 2H), ylmethyl)thiophene- 4.13 (d,J = 6.6 Hz, 2H), 3.09-2.83 (m, 4H), 2-carboxamide 2.47-2.40 (m, 1H),2.14-1.96 (m, 1H), 1.88- 1.69 (m, 1H), 1.69-1.54 (m, 1H), 1.37- 1.14 (m,1H) 345 N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (ESI(+))a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.49 (d, J = 7.0 Hz, 1H), m/e 338ylmethyl)-5-(1- 8.12 (s, 1H), 7.89 (s, 1H), 7.79 (s, 1H), 7.74 (M + H)⁺methyl-1H-pyrazol- (d, J = 3.8 Hz, 1H), 7.52 (d, J = 1.1 Hz, 1H),4-yl)thiophene-2- 7.40 (s, 1H), 7.21 (d, J = 3.8 Hz, 1H), 6.84carboxamide (dd, J = 7.0, 1.6 Hz, 1H), 4.48 (d, J = 5.9 Hz, 2H), 3.86(s, 3H) 363 N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.22(ESI(+)) a]pyridin-7- (t, J = 5.9 Hz, 1H), 8.50 (dd, J = 6.9, 0.8 Hz,m/e 338 ylmethyl)-5-(1- 1H), 7.92-7.86 (m, 2H), 7.53 (d, J = 1.2 Hz,(M + H)⁺ methyl-1H-pyrazol- 1H), 7.48 (d, J = 2.0 Hz, 1H), 7.45 (d, J =3.9 5-yl)thiophene-2- Hz, 1H), 7.41 (s, 1H), 6.86 (dd, J = 7.0, 1.7carboxamide Hz, 1H), 6.59 (d, J = 1.9 Hz, 1H), 4.51 (d, J = 5.9 Hz, 2H),3.98 (s, 3H) 395 N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03(ESI(+)) a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 6.9, 1.0 Hz,m/e 408 ylmethyl)-5-{1- 1H), 8.12 (s, 1H), 7.89 (t, J = 1.0 Hz, 1H),(M + H)⁺ [(2R)- 7.81 (s, 1H), 7.74 (d, J = 4.0 Hz, 1H), 7.52 (d,tetrahydrofuran-2- J = 1.5 Hz, 1H), 7.40 (s, 1H), 7.23 (d, J = 4.0ylmethyl]-1H- Hz, 1H), 6.85 (dd, J = 7.0, 1.7 Hz, 1H), 4.48 pyrazol-4-(d, J = 5.9 Hz, 2H), 4.26-4.04 (m, 3H), 3.82- yl}thiophene-2- 3.69 (m,1H), 3.69-3.57 (m, 1H), 2.00-1.85 carboxamide (m, 1H), 1.85-1.70 (m,2H), 1.70-1.52 (m, 1H) 397 N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δppm 9.02 (ESI(+)) a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 6.9,1.0 Hz, m/e 408 ylmethyl)-5-{1- 1H), 8.11 (d, J = 0.9 Hz, 1H), 7.89 (d,J = 0.9 (M + H)⁺ [(2S)- Hz, 1H), 7.80 (d, J = 0.9 Hz, 1H), 7.74 (d, J =tetrahydrofuran-2- 3.9 Hz, 1H), 7.52 (d, J = 1.2 Hz, 1H), 7.43-ylmethyl]-1H- 7.37 (m, 1H), 7.23 (d, J = 3.9 Hz, 1H), 6.85 pyrazol-4-(dd, J = 7.1, 1.7 Hz, 1H), 4.48 (d, J = 5.7 Hz, yl}thiophene-2- 2H),4.27-4.06 (m, 3H), 3.82-3.69 (m, 1H), carboxamide 3.69-3.58 (m, 1H),2.01-1.86 (m, 1H), 1.86- 1.69 (m, 2H), 1.69-1.52 (m, 1H) 410N-(imidazo[1,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (ESI(+))a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.49 (d, J = 6.7 Hz, 1H), m/e 408ylmethyl)-5-[1- 8.24 (s, 1H), 7.89 (s, 1H), 7.82 (s, 1H), 7.75 (M + H)⁺(tetrahydro-2H- (d, J = 3.9 Hz, 1H), 7.52 (d, J = 1.1 Hz, 1H),pyran-4-yl)-1H- 7.40 (s, 1H), 7.23 (d, J = 3.9 Hz, 1H), 6.85 pyrazol-4-(dd, J = 7.0, 1.7 Hz, 1H), 4.54-4.34 (m, 3H), yl]thiophene-2- 4.04-3.88(m, 2H), 3.47 (td, J = 11.3, 3.9 Hz, carboxamide 2H), 2.06-1.86 (m, 4H)465 N-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.05 (ESI(+))a]pyridin-7- (t, J = 6.0 Hz, 1H), 8.50 (d, J = 7.0 Hz, 1H), m/e 436ylmethyl)-5-{1-[(2- 8.03 (s, 1H), 7.90 (s, 1H), 7.80 (s, 1H), 7.75 (M +H)⁺ methyltetrahydro- (d, J = 3.8 Hz, 1H), 7.54 (d, J = 1.1 Hz, 1H),2H-pyran-2- 7.41 (s, 1H), 7.25 (d, J = 3.9 Hz, 1H), 6.86 yl)methyl]-1H-(dd, J = 7.0, 1.6 Hz, 1H), 4.49 (d, J = 5.9 Hz, pyrazol-4- 2H), 4.24 (d,J = 14.1 Hz, 1H), 4.10 (d, J = yl}thiophene-2- 14.0 Hz, 1H), 3.81-3.67(m, 1H), 3.65-3.52 carboxamide (m, 1H), 1.71-1.55 (m, 2H), 1.52-1.31 (m,4H), 1.07 (s, 3H) 466 tert-butyl 4-[(4-{5- ¹H NMR (300 MHz, DMSO-d₆) δppm 9.02 (ESI(+)) [(imidazo[1,2- (t, J = 6.0 Hz, 1H), 8.49 (dd, J = 7.1,1.0 Hz, m/e 521 a]pyridin-7- 1H), 8.14 (d, J = 0.8 Hz, 1H), 7.89 (s,1H), (M + H)⁺ ylmethyl)car- 7.81 (d, J = 0.9 Hz, 1H), 7.74 (d, J = 3.8Hz, bamoyl]thiophen-2-yl}- 1H), 7.52 (d, J = 1.3 Hz, 1H), 7.40 (s, 1H),1H-pyrazol-1- 7.22 (d, J = 3.9 Hz, 1H), 6.84 (dd, J = 7.1, 1.7yl)methyl]piperidine- Hz, 1H), 4.48 (d, J = 5.7 Hz, 2H), 4.02 (d, J =1-carboxylate 7.0 Hz, 2H), 3.92 (d, J = 13.2 Hz, 2H), 2.81- 2.57 (m,2H), 2.16-1.90 (m, 1H), 1.56-1.42 (m, 2H), 1.38 (s, 9H), 1.22-0.94 (m,2H) 475 5-[1- (ESI(+)) (cyclobutylmethyl)- m/e 392 1H-pyrazol-4-yl]-(M + H)⁺ N-(imidazo[1,2- a]pyridin-7- ylmethyl)thiophene- 2-carboxamide476 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 392 ylmethyl)-5-[1- (M +H)⁺ (tetrahydrofuran-2- ylmethyl)-1H- pyrazol-4-yl]furan- 2-carboxamide477 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 406 ylmethyl)-5-[1- (M +H)⁺ (tetrahydro-2H- pyran-2-ylmethyl)- 1H-pyrazol-4- yl]furan-2-carboxamide 478 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 392ylmethyl)-5-[1- (M + H)⁺ (tetrahydrofuran-3- ylmethyl)-1H-pyrazol-4-yl]furan- 2-carboxamide 479 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 406 ylmethyl)-5-[1- (M + H)⁺ (tetrahydro-2H-pyran-3-ylmethyl)- 1H-pyrazol-4- yl]furan-2- carboxamide 480N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 406 ylmethyl)-5-[1- (M + H)⁺(tetrahydro-2H- pyran-4-ylmethyl)- 1H-pyrazol-4- yl]furan-2- carboxamide481 5-[1- (ESI(+)) (cyclobutylmethyl)- m/e 376 1H-pyrazol-4-yl]- (M +H)⁺ N-(imidazo[1,2- a]pyridin-7- ylmethyl)furan-2- carboxamide 482N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 392 ylmethyl)-5-{1-[(3- (M +H)⁺ methyloxetan-3- yl)methyl]-1H- pyrazol-4-yl}furan- 2-carboxamide 4835-[1-(2-hydroxy-2- (ESI(+)) methylpropyl)-1H- m/e 380 pyrazol-4-yl]-N-(M + H)⁺ (imidazo[1,2- a]pyridin-7- ylmethyl)furan-2- carboxamide 8835-[1-(2,2- (ESI(+)) dimethylpropyl)- m/e 394 1H-pyrazol-4-yl]- (M + H)⁺N-(imidazo[1,2- a]pyridin-7- ylmethyl)thiophene- 2-carboxamide 884N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 472 ylmethyl)-5-[1- (M + H)⁺(tricyclo[3.3.1.1~3, 7~]dec-1- ylmethyl)-1H- pyrazol-4- yl]thiophene-2-carboxamide 885 5-(1-benzyl-1H- (ESI(+)) pyrazol-4-yl)-N- m/e 414(imidazo[1,2- (M + H)⁺ a]pyridin-7- ylmethyl)thiophene- 2-carboxamide886 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 474 ylmethyl)-5-[1-(2-(M + H)⁺ oxatricyclo[3.3.1.1~ 3,7~]dec-1- ylmethyl)-1H- pyrazol-4-yl]thiophene-2- carboxamide 1082 5-{1-[2,2-dimethyl- (ESI(+))3-(piperazin-1- m/e 478 yl)propyl]-1H- (M + H)⁺ pyrazol-4-yl}-N-(imidazo[1,2- a]pyridin-7- ylmethyl)thiophene- 2-carboxamide 10835-[1-(3-amino-2,2- (ESI(+)) dimethylpropyl)- m/e 409 1H-pyrazol-4-yl]-(M + H)⁺ N-(imidazo[1,2- a]pyridin-7- ylmethyl)thiophene- 2-carboxamide

Example 762-cyclopentyl-N-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}acetamideExample 76A N-(imidazo[1,2-a]pyridin-6-yl)-2-(4-nitrophenyl)acetamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-amine for 3-methylbutan-1-amine and2-(4-nitrophenyl)acetic acid for 4-nitrobenzoic acid.

Example 76B 2-(4-aminophenyl)-N-(imidazo[1,2-a]pyridin-6-yl)acetamide

The title compound was prepared as described in Example 1B, substitutingN-(imidazo[1,2-a]pyridin-6-yl)-2-(4-nitrophenyl)acetamide forN-isopentyl-4-nitrobenzamide.

Example 76C2-cyclopentyl-N-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}acetamide

The title compound was prepared as described in Example 52A,substituting 2-(4-aminophenyl)-N-(imidazo[1,2-a]pyridin-6-yl)acetamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.71 (s,1H), 9.83 (s, 1H), 9.55 (m, 1H), 8.38 (d, J=2.0 Hz, 1H), 8.08 (d, J=2.0Hz, 1H), 7.96-7.88 (m, 1H), 7.80-7.73 (m, 1H), 7.58-7.51 (m, 2H),7.29-7.23 (m, 2H), 3.67 (bs, 2H), 2.34-2.15 (m, 3H), 1.82-1.65 (m, 2H),1.67-1.41 (m, 4H), 1.26-1.10 (m, 2H); MS (ESI(+)) m/e 377 (M+H)⁺.

Example 77N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamideExample 77A tert-butyl4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)phenylcarbamate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(tert-butoxycarbonylamino)benzoic acid for 4-nitrobenzoic acid.

Example 77B 4-amino-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)phenylcarbamate fortert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 77CN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-2-ylacetyl)amino]benzamide

The title compound was prepared as described in Example 1A, substituting4-amino-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide for3-methylbutan-1-amine and 2-(tetrahydrofuran-2-yl)acetic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.14 (s, 1H), 8.93(t, J=5.8 Hz, 1H), 8.48-8.45 (m, 1H), 7.95 (s, 1H), 7.88-7.82 (m, 2H),7.71-7.64 (m, 2H), 7.53 (m, 7.55-7.48, 2H), 7.22 (dd, J=9.2, 1.7 Hz,1H), 4.45 (d, J=5.8 Hz, 2H), 4.23-4.12 (m, 1H), 3.82-3.72 (m, 1H),3.66-3.56 (m, 1H), 2.59-2.44 (m, 2H), 2.07-1.95 (m, 1H), 1.92-1.77 (m,2H), 1.60-1.47 (m, 1H); MS (ESI(+)) m/e 379 (M+H)⁺.

Example 78N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide

The title compound was prepared as described in Example 77, substituting2-(tetrahydrofuran-3-yl)acetic acid for 2-(tetrahydrofuran-2-yl)aceticacid in Example 77C. ¹H NMR (500 MHz, DMSO-d₆, Temp=90° C.) δ ppm 9.87(bs, 1H), 8.65-8.59 (m, 1H), 8.42 (s, 1H), 7.87 (s, 1H), 7.84-7.79 (m,2H), 7.66-7.61 (m, 2H), 7.52-7.45 (m, 2H), 7.21 (dd, J=9.2, 1.7 Hz, 1H),4.45 (d, J=5.8 Hz, 2H), 3.85-3.78 (m, 1H), 3.77-3.69 (m, 1H), 3.68-3.60(m, 1H), 3.38-3.31 (m, 1H), 2.64-2.54 (m, 1H), 2.45-2.40 (m, 2H),2.09-1.98 (m, 1H), 1.63-1.51 (m, 1H); MS (ESI(+)) m/e 379 (M+H)⁺.

Example 79N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide

The title compound was prepared as described in Example 77, substituting2-(tetrahydro-2H-pyran-4-yl)acetic acid for2-(tetrahydrofuran-2-yl)acetic acid in Example 77C. ¹H NMR (500 MHz,DMSO-d₆, Temp=90° C.) δ ppm 9.84 (bs, 1H), 8.67-8.60 (m, 1H), 8.42 (s,1H), 7.87 (s, 1H), 7.85-7.79 (m, 2H), 7.67-7.61 (m, 2H), 7.52-7.45 (m,2H), 7.21 (dd, J=9.2, 1.7 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 3.85-3.77 (m,2H), 3.35-3.26 (m, 2H), 2.28 (d, J=7.0 Hz, 2H), 2.07-1.96 (m, 1H),1.65-1.57 (m, 2H), 1.31-1.22 (m, 2H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 80N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[(morpholin-4-ylacetyl)amino]benzamide

The title compound was prepared as described in Example 77, substituting2-morpholinoacetic acid for 2-(tetrahydrofuran-2-yl)acetic acid inExample 77C. ¹H NMR (500 MHz, DMSO-d₆, Temp=90° C.) δ ppm 9.70 (bs, 1H),8.69-8.63 (m, 1H), 8.42 (s, 1H), 7.90-7.81 (m, 3H), 7.70-7.65 (m, 2H),7.53-7.45 (m, 2H), 7.21 (dd, J=9.3, 1.7 Hz, 1H), 4.46 (d, J=5.8 Hz, 2H),3.67-3.61 (m, 4H), 3.14 (s, 2H), 2.56-2.52 (m, 4H); MS (ESI(+)) m/e 394(M+H)⁺.

Example 814-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 77, substituting4-cyclopentylbutanoic acid for 2-(tetrahydrofuran-2-yl)acetic acid inExample 77C. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.10 (s, 1H), 8.92 (t,J=5.8 Hz, 1H), 8.46 (dd, J=1.9, 0.9 Hz, 1H), 7.95 (dd, J=1.2, 0.6 Hz,1H), 7.87-7.81 (m, 2H), 7.70-7.64 (m, 2H), 7.55-7.49 (m, 2H), 7.22 (dd,J=9.2, 1.7 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 2.37-2.30 (m, 2H), 1.81-1.68(m, 3H), 1.64-1.41 (m, 6H), 1.19-1.02 (m, 2H); MS (ESI(+)) m/e 391(M+H)⁺.

Example 82N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[(propan-2-yloxy)acetyl]amino}benzamide

The title compound was prepared as described in Example 77, substituting2-isopropoxyacetic acid for 2-(tetrahydrofuran-2-yl)acetic acid inExample 77C. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.78 (s, 1H), 8.95 (t,J=5.8 Hz, 1H), 8.49-8.44 (m, 1H), 7.97-7.93 (m, 1H), 7.89-7.83 (m, 2H),7.78-7.72 (m, 2H), 7.56-7.50 (m, 2H), 7.22 (dd, J=9.2, 1.7 Hz, 1H), 4.46(d, J=5.8 Hz, 2H), 4.04 (s, 2H), 3.75-3.64 (m, 1H), 1.17 (d, J=6.1 Hz,6H); MS (ESI(+)) m/e 367 391 (M+H)⁺.

Example 83 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylateExample 83A 4-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-bromobenzoic acid for 4-nitrobenzoic acid.

Example 83B tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 4-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=5.9 Hz, 1H),8.49-8.45 (m, 1H), 7.97-7.93 (m, 1H), 7.91-7.84 (m, 2H), 7.61-7.48 (m,4H), 7.22 (dd, J=9.3, 1.7 Hz, 1H), 6.32-6.25 (m, 1H), 4.47 (d, J=5.8 Hz,2H), 4.05-3.99 (m, 2H), 3.58-3.50 (m, 2H), 2.55-2.44 (m, 2H), 1.43 (s,9H); MS (ESI(+)) m/e 433 (M+H)⁺.

Example 84N-{4-[(cyclopentylacetyl)amino]benzyl}imidazo[1,2-a]pyridine-6-carboxamideExample 84A N-(4-nitrobenzyl)imidazo[1,2-a]pyridine-6-carboxamide

The title compound was prepared as described in Example 1A, substituting(4-nitrophenyl)methanamine for 3-methylbutan-1-amine andimidazo[1,2-a]pyridine-6-carboxylic acid for 4-nitrobenzoic acid.

Example 84B N-(4-aminobenzyl)imidazo[1,2-a]pyridine-6-carboxamide

The title compound was prepared as described in Example 1B, substitutingN-(4-nitrobenzyl)imidazo[1,2-a]pyridine-6-carboxamide forN-isopentyl-4-nitrobenzamide.

Example 84CN-{4-[(cyclopentylacetyl)amino]benzyl}imidazo[1,2-a]pyridine-6-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(4-aminobenzyl)imidazo[1,2-a]pyridine-6-carboxamide for3-methylbutan-1-amine and 2-cyclopentylacetic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.80 (s, 1H), 9.16-9.11 (m, 1H),9.04 (t, J=5.9 Hz, 1H), 8.08-8.03 (m, 1H), 7.76-7.57 (m, 3H), 7.58-7.50(m, 2H), 7.29-7.22 (m, 2H), 4.44 (d, J=5.8 Hz, 2H), 2.33-2.14 (m, 3H),1.81-1.67 (m, 2H), 1.66-1.42 (m, 4H), 1.27-1.09 (m, 2H); MS (ESI(+)) m/e377 (M+H)⁺.

Example 85N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-1,3-thiazole-5-carboxamideExample 85A2-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and2-bromothiazole-5-carboxamide for 4-nitrobenzoic acid.

Example 85BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 53B, substituting2,3,4,5-tetrahydro-1H-benzo[d]azepine for 4-cyanobenzylamine and2-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiazole-5-carboxamide for2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 8.78 (t, J=5.8 Hz, 1H), 8.44 (s, 1H), 7.95 (s,1H), 7.86 (s, 1H), 7.48-7.56 (m, 2H), 7.08-7.22 (m, 5H), 4.38 (d, J=5.9Hz, 2H), 3.67-3.78 (m, 4H), 2.89-3.01 (m, 4H); MS (ESI(+)) m/e 402(M+H)⁺.

Example 86N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-(3-phenylpyrrolidin-1-yl)-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 85, substituting3-phenylpyrrolidine for 2,3,4,5-tetrahydro-1H-benzo[d]azepine in Example85B. ¹H NMR (400 MHz, DMSO-d₆) δ 8.75 (dd, J=5.8, 5.6 Hz, 1H), 8.44 (s,1H), 7.95 (s, 1H), 7.86 (s, 1H), 7.56-7.50 (m, 2H), 7.35-7.31 (m, 2H),7.29-7.21 (m, 2H), 7.18 (dd, J=8.4, 4.7 Hz, 1H), 4.45 (s, 1H), 4.38 (d,J=5.8 Hz, 2H), 3.92-3.83 (m, 2H), 3.62-3.45 (m, 2H), 2.68-2.62 (m, 1H),2.42-2.30 (m, 1H), 2.20-2.07 (m, 1H). MS (ESI)(+)) m/e 404 (M+H)⁺.

Example 87N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 85, substituting3-methylbutan-1-amine for 2,3,4,5-tetrahydro-1H-benzo[d]azepine inExample 85B. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.67 (t, J=5.9 Hz, 1H),8.42 (s, 1H), 8.08 (t, J=5.4 Hz, 1H), 7.94 (s, 1H), 7.71 (s, 1H),7.49-7.55 (m, 2H), 7.16 (dd, J=9.3, 1.6 Hz, 1H), 4.36 (d, J=5.9 Hz, 2H),3.17-3.26 (m, 2H), 1.61 (dq, J=6.7 Hz, 1H), 1.41 (q, J=7.0 Hz, 2H), 0.87(d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 344 (M+H)⁺.

Example 882-(1,3-dihydro-2H-isoindol-2-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 85, substitutingisoindoline for 2,3,4,5-tetrahydro-1H-benzo[d]azepine in Example 85B. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 8.81 (t, J=5.9 Hz, 1H), 8.45 (s, 1H),7.89-7.99 (m, 2H), 7.49-7.56 (m, 2H), 7.37-7.45 (m, 2H), 7.30-7.37 (m,2H), 7.19 (dd, J=9.3, 1.5 Hz, 1H), 4.76 (s, 4H), 4.40 (d, J=5.7 Hz, 2H);MS (ESI(+)) m/e 376 (M+H)⁺.

Example 89 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylcarbamoyl)amino]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.98-8.94(m, 1H), 8.67 (s, 1H), 8.64 (s, 1H), 7.97-7.93 (m, 1H), 7.54-7.48 (m,2H), 7.42-7.36 (m, 2H), 7.19-7.12 (m, 2H), 7.08 (dd, J=9.5, 2.1 Hz, 1H),4.14-3.99 (m, 2H), 2.89-2.56 (m, 3H), 1.77-1.69 (m, 2H), 1.52-1.36 (m,11H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 90N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamideExample 90AN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(1,2,3,6-tetrahydropyridin-4-yl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 90BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(1,2,3,6-tetrahydropyridin-4-yl)benzamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.75-8.67 (m, 1H), 8.43 (s,1H), 7.89-7.83 (m, 3H), 7.54-7.43 (m, 4H), 7.21 (dd, J=9.2, 1.7 Hz, 1H),6.29-6.23 (m, 1H), 4.47 (d, J=5.8 Hz, 2H), 4.19-4.13 (m, 2H), 3.70 (t,J=5.7 Hz, 2H), 2.95-2.84 (m, 1H), 2.57-2.49 (m, 2H), 1.04 (d, J=6.7 Hz,6H); MS (ESI(+)) m/e 403 (M+H)⁺.

TABLE 7 The following Examples were prepared essentially as described inExample 90, substituting the appropriate carboxylic acid for isobutyricacid in Example 90B. Ex Name ¹H NMR MS 91 4-[1-(2-hydroxy-2- (ESI(+))methylpropanoyl)- m/e 419 1,2,3,6- (M + H)⁺ tetrahydropyridin-4-yl]-N-(imidazo[1,2- a]pyridin-6- ylmethyl)benzamide 92 N-(imidazo[1,2-(ESI(+)) a]pyridin-6- m/e 460 ylmethyl)-4-[1- (M + H)⁺ (morpholin-4-ylacetyl)-1,2,3,6- tetrahydropyridin-4- yl]benzamide 93 N-(imidazo[1,2-(ESI(+)) a]pyridin-6- m/e 459 ylmethyl)-4-[1- (M + H)⁺ (tetrahydro-2H-pyran-4-ylacetyl)- 1,2,3,6- tetrahydropyridin-4- yl]benzamide 94N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 445 ylmethyl)-4-[1- (M + H)⁺(tetrahydrofuran-3- ylacetyl)-1,2,3,6- tetrahydropyridin-4- yl]benzamide95 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 445 ylmethyl)-4-[1- (M +H)⁺ (tetrahydrofuran-2- ylacetyl)-1,2,3,6- tetrahydropyridin-4-yl]benzamide 96 N-(imidazo[1,2- (ESI(+)) a]pyridin-6- m/e 459ylmethyl)-4-{1-[3- (M + H)⁺ (tetrahydrofuran-2- yl)propanoyl]- 1,2,3,6-tetrahydropyridin-4- yl}benzamide 97 4-[1- ¹H NMR (300 MHz, methanol-d₄)δ ppm 8.81- (ESI(+)) (cyclopentylacetyl)- 8.76 (m, 1H), 8.21 (m, 1H),8.05-7.98 (m, m/e 443 1,2,3,6- 2H), 7.97-7.79 (m, 3H), 7.59-7.53 (m,2H), (M + H)⁺ tetrahydropyridin-4- 6.31-6.23 (m, 1H), 4.74-4.65 (m, 2H),4.29- yl]-N-(imidazo[1,2- 4.19 (m, 2H), 3.85-3.75 (m, 2H), 2.71-a]pyridin-6- 2.41 (m, 4H), 2.33-2.14 (m, 1H), 1.92-1.74ylmethyl)benzamide (m, 2H), 1.76-1.49 (m, 4H), 1.32-1.13 (m, 2H) 98N-(imidazo[1,2- ¹H NMR (300 MHz, methanol-d₄) δ ppm 8.81- (ESI(+))a]pyridin-6- 8.76 (m, 1H), 8.21 (m, 1H), 8.05-7.98 (m, m/e 443ylmethyl)-4-{1- 2H), 7.95-7.83 (m, 3H), 7.61-7.51 (m, 2H), (M + H)⁺[(propan-2- 6.31-6.22 (m, 1H), 4.74-4.68 (m, 2H), 4.32- yloxy)acetyl]-4.17 (m, 4H), 3.90-3.64 (m, 3H), 2.73- 1,2,3,6- 2.53 (m, 2H), 1.25-1.16(m, 6H) tetrahydropyridin-4- yl}benzamide 99 N-(imidazo[1,2- ¹H NMR (300MHz, methanol-d₄) δ ppm 8.81- (ESI(+)) a]pyridin-6- 8.77 (m, 1H),8.22-8.20 (m, 1H), 8.02- m/e 431 ylmethyl)-4-[1- 7.99 (m, 2H), 7.97-7.82(m, 3H), 7.59-7.53 (M + H)⁺ (tetrahydrofuran-2- (m, 2H), 6.31-6.23 (m,1H), 4.82-4.74 (m, ylcarbonyl)-1,2,3,6- 1H), 4.70 (s, 2H), 4.40-4.11 (m,2H), 4.01- tetrahydropyridin-4- 3.71 (m, 4H), 2.74-2.52 (m, 2H),2.30-2.17 yl]benzamide (m, 1H), 2.17-1.84 (m, 3H) 100 N-(imidazo[1,2- ¹HNMR (300 MHz, methanol-d₄) δ ppm 8.81- (ESI(+)) a]pyridin-6- 8.77 (m,1H), 8.24-8.17 (m, 1H), 8.05- m/e 431 ylmethyl)-4-[1- 7.97 (m, 2H),7.97-7.82 (m, 3H), 7.59-7.53 (M + H)⁺ (tetrahydrofuran-3- (m, 2H),6.31-6.25 (m, 1H), 4.72 (s, 2H), ylcarbonyl)-1,2,3,6- 4.35-4.21 (m, 2H),4.06-3.93 (m, 1H), 3.95- tetrahydropyridin-4- 3.76 (m, 5H), 3.60-3.42(m, 1H), 2.71- yl]benzamide 2.52 (m, 2H), 2.27-2.02 (m, 2H) 101N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.81- (ESI(+))a]pyridin-6- 8.78 (m, 1H), 8.23-8.19 (m, 1H), 8.05- m/e 828ylmethyl)-4-[1- 7.98 (m, 2H), 7.93-7.84 (m, 3H), 7.59-7.53 (M + H)⁺(tetrahydro-2H- (m, 2H), 6.31-6.25 (m, 1H), 4.70 (s, 2H), pyran-4-4.36-4.30 (m, 1H), 4.25-4.19 (m, 1H), 4.02- ylcarbonyl)-1,2,3,6- 3.93(m, 2H), 3.87-3.78 (m, 2H), 3.59- tetrahydropyridin-4- 3.46 (m, 2H),3.10-2.92 (m, 1H), 2.70-2.53 yl]benzamide (m, 2H), 1.91-1.72 (m, 2H),1.73-1.57 (m, 2H) 102 4-[1-(1,4-dioxan-2- ¹H NMR (400 MHz, methanol-d₄)δ ppm 8.79 (ESI(+)) ylcarbonyl)-1,2,3,6- (s, 1H), 8.23-8.20 (m, 1H),8.04-7.99 (m, m/e 447 tetrahydropyridin-4- 2H), 7.93-7.84 (m, 3H),7.59-7.53 (m, 2H), (M + H)⁺ yl]-N-(imidazo[1,2- 6.29-6.23 (m, 1H),4.73-4.67 (m, 2H), 4.53- a]pyridin-6- 4.06 (m, 3H), 3.96-3.59 (m, 8H),2.76- ylmethyl)benzamide 2.53 (m, 2H) 103 N-(imidazo[1,2- ¹H NMR (400MHz, methanol-d₄) δ ppm 8.79 (ESI(+)) a]pyridin-6- (s, 1H), 8.24-8.19(m, 1H), 8.01 (m, 2H), m/e 449 ylmethyl)-4-{1-[(2- 7.97-7.82 (m, 3H),7.59-7.53 (m, 2H), 6.31- (M + H)⁺ methoxyethoxy)acetyl]- 6.23 (m, 1H),4.76-4.69 (m, 2H), 4.35- 1,2,3,6- 4.26 (m, 2H), 4.25-4.19 (m, 2H),3.86-3.62 tetrahydropyridin-4- (m, 4H), 3.61-3.54 (m, 2H), 3.35 (s, 3H),yl}benzamide 2.72-2.54 (m, 2H) 104 4-(1-benzoyl- ¹H NMR (400 MHz,DMSO-d₆, Temp = 90° C.) (ESI(+)) 1,2,3,6- δ ppm 8.89-8.82 (m, 1H), 8.73(s, 1H), 8.22 m/e 437 tetrahydropyridin-4- (d, J = 1.9 Hz, 1H), 7.96 (d,J = 1.9 Hz, 1H), (M + H)⁺ yl)-N-(imidazo[1,2- 7.90-7.75 (m, 4H),7.56-7.49 (m, 2H), 7.49- a]pyridin-6- 7.37 (m, 5H), 6.27 (bs, 1H), 4.58(d, J = 5.8 ylmethyl)benzamide Hz, 2H), 4.23-4.17 (m, 2H), 3.72-3.65 (m,2H), 2.61-2.53 (m, 2H) 105 4-{1-[(4,4- ¹H NMR (400 MHz, DMSO-d₆, Temp =90° C.) (ESI(+)) difluorocyclohexyl) δ ppm 8.90-8.83 (m, 1H), 8.74 (s,1H), 8.22 m/e 479 carbonyl]-1,2,3,6- (d, J = 1.9 Hz, 1H), 7.97 (d, J =1.9 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.90-7.75 (m, 4H), 7.54-7.48(m, 2H), 6.30- yl}-N-(imidazo[1,2- 6.24 (m, 1H), 4.58 (d, J = 5.8 Hz,2H), 4.21- a]pyridin-6- 4.15 (m, 2H), 3.77-3.69 (m, 2H), 2.91-ylmethyl)benzamide 2.79 (m, 1H), 2.58-2.51 (m, 2H), 2.12-2.00 (m, 2H),2.00-1.59 (m, 6H)

Example 1061-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}ureaExample 106A1-(imidazo[1,2-a]pyridin-6-yl)-3-(4-(piperidin-4-yl)phenyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 106B1-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 1A, substituting1-(imidazo[1,2-a]pyridin-6-yl)-3-(4-(piperidin-4-yl)phenyl)urea for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.86-8.81 (m, 1H), 8.41 (s,1H), 8.38 (s, 1H), 7.86 (s, 1H), 7.50-7.42 (m, 2H), 7.40-7.34 (m, 2H),7.18-7.12 (m, 2H), 7.12-7.06 (m, 1H), 4.41-4.18 (m, 2H), 2.95-2.64 (m,4H), 1.87-1.78 (m, 2H), 1.56-1.38 (m, 2H), 1.03 (d, J=6.7 Hz, 6H); MS(ESI(+)) m/e 406 (M+H)⁺.

Example 1082-(3,4-dihydroisoquinolin-2(1H)-yl)-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 85, substituting1,2,3,4-tetrahydroisoquinoline for 2,3,4,5-tetrahydro-1H-benzo[d]azepinein Example 85B. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.81 (t, J=5.8 Hz, 1H),8.47 (s, 1H), 7.98 (s, 1H), 7.89 (s, 1H), 7.48-7.63 (m, 2H), 7.13-7.32(m, 5H), 4.65 (s, 2H), 4.39 (d, J=5.9 Hz, 2H), 3.73 (t, J=6.0 Hz, 2H),2.94 (t, J=6.0 Hz, 2H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 1091-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 106,substituting tetrahydro-2H-pyran-4-carboxylic acid for isobutyric acidin Example 106B. ¹H NMR (400 MHz, methanol-d₄) δ ppm 9.37-9.33 (m, 1H),8.22-8.17 (m, 1H), 7.97 (d, J=2.1 Hz, 1H), 7.89-7.77 (m, 2H), 7.44-7.38(m, 2H), 7.24-7.18 (m, 2H), 4.73-4.64 (m, 1H), 4.25-4.15 (m, 1H),4.01-3.93 (m, 2H), 3.57-3.46 (m, 2H), 3.27-3.17 (m, 1H), 3.06-2.95 (m,1H), 2.87-2.66 (m, 2H), 2.00-1.70 (m, 4H), 1.70-1.48 (m, 4H); MS(ESI(+)) m/e 448 (M+H)⁺.

Example 1101-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 106,substituting 2-(tetrahydrofuran-3-yl)acetic acid for isobutyric acid inExample 106B. ¹H NMR (400 MHz, methanol-d₄) δ ppm 9.37-9.32 (m, 1H),8.21-8.17 (m, 1H), 7.97 (d, J=2.1 Hz, 1H), 7.88-7.76 (m, 2H), 7.44-7.38(m, 2H), 7.23-7.18 (m, 2H), 4.71-4.62 (m, 1H), 4.14-4.05 (m, 1H),3.95-3.82 (m, 2H), 3.81-3.70 (m, 1H), 3.47-3.35 (m, 1H), 3.25-3.12 (m,1H), 2.86-2.48 (m, 5H), 2.22-2.07 (m, 1H), 1.95-1.83 (m, 2H), 1.74-1.46(m, 3H); MS (ESI(+)) m/e 448 (M+H)⁺.

Example 1111-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 106,substituting 2-(tetrahydrofuran-2-yl)acetic acid for isobutyric acid inExample 106B. ¹H NMR (400 MHz, methanol-d₄) δ ppm 9.37-9.32 (m, 1H),8.21-8.17 (m, 1H), 7.99-7.95 (m, 1H), 7.88-7.77 (m, 2H), 7.44-7.38 (m,2H), 7.23-7.17 (m, 2H), 4.73-4.63 (m, 1H), 4.33-4.20 (m, 1H), 4.19-4.10(m, 1H), 3.92-3.83 (m, 1H), 3.79-3.69 (m, 1H), 3.26-3.14 (m, 1H),2.87-2.65 (m, 3H), 2.63-2.47 (m, 1H), 2.19-2.06 (m, 1H), 2.01-1.81 (m,4H), 1.77-1.50 (m, 3H); MS (ESI(+)) m/e 448 (M+H)⁺.

Example 1121-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-imidazo[1,2-a]pyridin-6-ylurea

The title compound was prepared as described in Example 106,substituting benzoic acid for isobutyric acid in Example 106B. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 8.87-8.81 (m, 1H), 8.38 (bs, 1H), 8.38 (bs,1H), 7.86 (s, 1H), 7.51-7.34 (m, 9H), 7.21-7.14 (m, 2H), 7.09 (dd,J=9.5, 2.0 Hz, 1H), 4.34-3.97 (m, 2H), 3.08-2.95 (m, 2H), 2.83-2.71 (m,1H), 1.85-1.77 (m, 2H), 1.66-1.50 (m, 2H); MS (ESI(+)) m/e 440 (M+H)⁺.

Example 1131-imidazo[1,2-a]pyridin-6-yl-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 106,substituting tetrahydrofuran-2-carboxylic acid for isobutyric acid inExample 106B. ¹H NMR (400 MHz, methanol-d₄) δ ppm 9.38-9.33 (m, 1H),8.21-8.16 (m, 1H), 8.00-7.95 (m, 1H), 7.88-7.77 (m, 2H), 7.44-7.38 (m,2H), 7.23-7.17 (m, 2H), 4.83-4.73 (m, 1H), 4.69-4.60 (m, 1H), 4.22-4.11(m, 1H), 4.01-3.90 (m, 1H), 3.91-3.82 (m, 1H), 3.26-3.12 (m, 1H),2.87-2.68 (m, 2H), 2.31-2.14 (m, 1H), 2.12-1.75 (m, 5H), 1.77-1.50 (m,2H); MS (ESI(+)) m/e 434 (M+H)⁺.

Example 114 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yloxy)benzoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.40 (s, 1H),7.86-7.79 (m, 3H), 7.52 (t, J=5.4 Hz, 2H), 7.34 (dd, J=9.3, 1.7 Hz, 1H),7.06-6.99 (m, 2H), 4.72-4.60 (m, 1H), 4.56 (s, 2H), 3.77-3.65 (m, 2H),3.41-3.30 (m, 2H), 2.03-1.90 (m, 2H), 1.76-1.59 (m, 2H), 1.46 (s, 9H);MS (ESI(+)) m/e 451 (M+H)⁺.

Example 115N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamideExample 115A2-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and2-bromothiazole-5-carboxylic acid for 4-nitrobenzoic acid.

Example 115BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-((tetrahydrofuran-2-yl)methylamino)thiazole-5-carboxamide

The title compound was prepared as in Example 53B, substituting(tetrahydrofuran-2-yl)methanamine for 4-cyanobenzylamine and2-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiazole-5-carboxamide for2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide.

Example 115CN-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[{[2-(propan-2-yloxy)ethyl]carbamoyl}(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1C, substituting2-isopropoxyethanamine for 4-amino-N-isopentylbenzamide andN-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-((tetrahydrofuran-2-yl)methylamino)thiazole-5-carboxamidefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (400 MHz, CDCl₃) δ ppm 8.52(s, 1H), 8.21 (d, J=9.0 Hz, 1H), 7.96 (s, 1H), 7.89 (d, J⁼1.5 Hz, 1H),7.86-7.80 (m, 1H), 7.78 (d, J=9.5 Hz, 1H), 7.73 (s, 1H), 6.96-6.86 (m,1H), 4.74-4.60 (m, 2H), 4.50-4.38 (m, 1H), 4.26 (ddd, J=4.4, 2.2, 0.6Hz, 1H), 4.07-3.90 (m, 2H), 3.85-3.74 (m, 1H), 3.63 (dd, J=12.2, 6.1 Hz,1H), 3.60-3.53 (m, 2H), 3.53-3.41 (m, 2H), 1.95 (dd, J=7.8, 6.9 Hz, 3H),1.63-1.56 (m, 1H), 1.18 (dd, J=6.1, 1.2 Hz, 6H); (APCI(+)) m/e 487(M+H)⁺.

TABLE 8 The following Examples were prepared essentially as described inExample 115, substituting the appropriate amine in Example 115B and theappropriate amine for 2-isopropoxyethanamine in Example 115C. Ex Name ¹HNMR MS 138 N-(imidazo[1,2- ¹H NMR (400 MHz, CDCl₃) δ ppm 8.09 (d,(APCI(+)) a]pyridin-7- J = 7.0 Hz, 1H), 7.86 (d, J = 14.0 Hz, 2H), m/e459 ylmethyl)-2-{[(2- 7.62 (d, J = 0.8 Hz, 1H), 7.54 (d, J = 9.1 Hz,(M + H)+ methoxyethyl)carbam- 2H), 6.84 (dd, J = 7.0, 1.4 Hz, 1H), 6.27(t, oyl](tetrahydrofuran- J = 5.8 Hz, 1H), 4.63 (d, J = 6.0 Hz, 2H),2-ylmethyl)amino}- 4.44 (d, J = 14.3 Hz, 1H), 4.29 (q, J = 7.31,3-thiazole-5- Hz, 1H), 4.05 (dd, J = 15.4, 7.2 Hz, 1H), carboxamide3.92 (dd, J = 15.2, 7.2 Hz, 1H), 3.86-3.72 (m, 1H), 3.58-3.51 (m, 2H),3.48 (dd, J = 9.2, 3.8 Hz, 3H), 3.39 (s, 3H), 2.14 (dt, J = 12.4, 6.3Hz, 1H), 2.05-1.86 (m, 2H) 141 N-(imidazo[1,2- ¹H NMR (400 MHz,methanol-d₄) δ ppm (APCI(+)) a]pyridin-6- 8.78 (s, 1H), 8.22 (d, J = 2.1Hz, 1H), 8.03 m/e 459 ylmethyl)-2-{[(2- (d, J = 2.1 Hz, 1H), 7.99 (d, J= 9.8 Hz, (M + H)⁺ methoxyethyl)carbam- 2H), 7.91 (d, J = 9.3 Hz, 1H),4.65 (s, 2H), oyl](tetrahydrofuran- 4.24 (dd, J = 15.2, 7.6 Hz, 1H),4.12 (dd, J = 3-ylmethyl)amino}- 15.2, 7.9 Hz, 1H), 3.93 (td, J = 8.1,5.8 1,3-thiazole-5- Hz, 1H), 3.79-3.67 (m, 2H), 3.60 (dd, J =carboxamide 8.7, 5.2 Hz, 1H), 3.55-3.45 (m, 4H), 3.36 (s, 3H), 2.85-2.75(m, 1H), 2.00 (td, J = 13.4, 7.8 Hz, 1H), 1.72 (dt, J = 20.1, 6.3 Hz,1H) 151 N-(imidazo[1,2- ¹H NMR (500 MHz, methanol-d₄) δ ppm (APCI(+))a]pyridin-6- 8.77 (s, 1H), 8.21 (d, J = 2.0 Hz, 1H), 8.02 m/e 473ylmethyl)-2-{[(2- (d, J = 2.1 Hz, 1H), 7.99 (dd, J = 9.3, 1.4 (M + H)⁺methoxyethyl)carbam- Hz, 1H), 7.97 (s, 1H), 7.90 (d, J = 9.3 Hz,oyl](tetrahydro- 1H), 4.65 (s, 2H), 4.07 (d, J = 7.6 Hz, 2H),2H-pyran-4- 3.92 (dd, J = 11.5, 3.0 Hz, 2H), 3.52 (dd, J =ylmethyl)amino}- 8.3, 3.1 Hz, 2H), 3.47 (dd, J = 8.1, 3.0 Hz,1,3-thiazole-5- 2H), 3.36 (s, 3H), 3.36-3.32 (m, 2H), 2.14 carboxamide(ddd, J = 15.4, 7.7, 3.8 Hz, 1H), 1.54 (d, J = 11.2 Hz, 2H), 1.42 (qd, J= 12.1, 4.4 Hz, 2H) 152 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δppm (APCI(+)) a]pyridin-6- 8.78 (s, 1H), 8.22 (d, J = 2.1 Hz, 1H), 8.03m/e 501 ylmethyl)-2-[{[2- (d, J = 2.1 Hz, 1H), 8.01-7.97 (m, 2H), (M +H)⁺ (propan-2- 7.91 (d, J = 9.3 Hz, 1H), 4.65 (s, 2H), 4.06yloxy)ethyl]carbam- (d, J = 7.6 Hz, 2H), 3.92 (dd, J = 11.4, 3.0oyl}(tetrahydro-2H- Hz, 2H), 3.63 (dt, J = 12.2, 6.1 Hz, 1H), pyran-4-3.57 (dd, J = 10.1, 4.5 Hz, 2H), 3.45 (t, J = ylmethyl)amino]- 5.5 Hz,2H), 3.35 (dd, J = 11.6, 1.7 Hz, 2H), 1,3-thiazole-5- 2.16 (ddd, J =11.4, 7.6, 3.8 Hz, 1H), 1.55 carboxamide (dd, J = 12.6, 1.5 Hz, 2H),1.42 (qd, J = 12.1, 4.4 Hz, 2H), 1.16 (d, J = 6.1 Hz, 6H) 153N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ ppm (APCI(+))a]pyridin-6- 8.70 (s, 1H), 8.14 (d, J = 2.1 Hz, 1H), 7.95 m/e 459ylmethyl)-2-{[(2- (d, J = 2.2 Hz, 1H), 7.91 (dd, J = 9.4, 1.5 (M + H)⁺methoxyethyl)carbam- Hz, 1H), 7.88 (s, 1H), 7.82 (d, J = 9.3 Hz,oyl][(2R)- 1H), 4.57 (s, 2H), 4.33 (dd, J = 15.4, 1.8 tetrahydrofuran-2-Hz, 1H), 4.17 (dd, J = 11.3, 4.9 Hz, 1H), ylmethyl]amino}- 4.00 (dd, J =15.4, 7.7 Hz, 1H), 3.86 (dd, J = 1,3-thiazole-5- 15.2, 7.0 Hz, 1H), 3.71(td, J = 7.8, 5.8 carboxamide Hz, 1H), 3.52-3.39 (m, 2H), 3.38-3.32 (m,2H), 3.30 (s, 3H), 2.11-1.95 (m, 1H), 1.95-1.77 (m, 2H), 1.66-1.48 (m,1H), 0.99-0.87 (m, 1H) 154 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄)δ ppm (APCI(+)) a]pyridin-6- 8.77 (s, 1H), 8.21 (d, J = 2.1 Hz, 1H),8.02 m/e 487 ylmethyl)-2-({[2- (d, J = 2.1 Hz, 1H), 7.98 (dd, J = 9.4,1.2 (M + H)⁺ (propan-2- Hz, 1H), 7.96 (s, 1H), 7.90 (d, J = 9.3 Hz,yloxy)ethyl]carbam- 1H), 4.64 (s, 2H), 4.41 (dd, J = 15.4, 1.6oyl}[(2R)- Hz, 1H), 4.29-4.21 (m, 1H), 4.07 (dd, J = tetrahydrofuran-2-15.4, 7.6 Hz, 1H), 3.96 (dd, J = 15.0, 7.1 ylmethyl]amino)- Hz, 1H),3.77 (dd, J = 14.0, 7.7 Hz, 1H), 1,3-thiazole-5- 3.64 (dt, J = 12.2, 6.1Hz, 1H), 3.57 (t, J = carboxamide 5.0 Hz, 2H), 3.41 (t, J = 5.3 Hz, 2H),2.15- 2.03 (m, 1H), 2.00-1.87 (m, 2H), 1.64 (dq, J = 12.4, 8.2 Hz, 1H),1.16 (d, J = 6.1 Hz, 6H) 155 N-(imidazo[1,2- ¹H NMR (400 MHz,methanol-d₄) δ ppm (APCI(+)) a]pyridin-6- 8.78 (s, 1H), 8.21 (d, J = 2.1Hz, 1H), 8.03 m/e 459 ylmethyl)-2-{[(2- (d, J = 2.1 Hz, 1H), 8.01-7.97(m, 1H), (M + H)⁺ methoxyethyl)carbam- 7.96 (s, 1H), 7.90 (d, J = 9.3Hz, 1H), 4.64 oyl][(2S)- (s, 2H), 4.41 (d, J = 15.4 Hz, 1H), 4.26 (q, J= tetrahydrofuran-2- 6.4 Hz, 1H), 4.08 (dd, J = 15.4, 7.7 Hz,ylmethyl]amino}- 1H), 3.94 (dd, J = 15.1, 7.1 Hz, 1H), 3.791,3-thiazole-5- (dd, J = 13.7, 7.7 Hz, 1H), 3.53 (dt, J = 7.4,carboxamide 4.5 Hz, 2H), 3.43 (t, J = 5.2 Hz, 2H), 3.38 (s, 3H), 2.11(td, J = 12.3, 7.2 Hz, 1H), 2.01- 1.85 (m, 2H), 1.65 (dq, J = 12.2, 8.2Hz, 1H) 156 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ ppm(APCI(+)) a]pyridin-6- 8.78 (s, 1H), 8.22 (d, J = 2.1 Hz, 1H), 8.03 m/e487 ylmethyl)-2-({[2- (d, J = 2.1 Hz, 1H), 7.99 (dd, J = 9.3, 1.4 (M +H)⁺ (propan-2- Hz, 1H), 7.96 (s, 1H), 7.91 (d, J = 9.3 Hz,yloxy)ethyl]carbam- 1H), 4.65 (s, 2H), 4.41 (dd, J = 15.4, 1.8oyl}[(2S)- Hz, 1H), 4.31-4.22 (m, 1H), 4.08 (dd, J = tetrahydrofuran-2-15.4, 7.6 Hz, 1H), 3.96 (dd, J = 15.1, 7.0 ylmethyl]amino)- Hz, 1H),3.78 (dd, J = 14.0, 7.7 Hz, 1H), 1,3-thiazole-5- 3.65 (dt, J = 12.1, 6.1Hz, 1H), 3.57 (t, J = carboxamide 4.9 Hz, 2H), 3.41 (t, J = 5.3 Hz, 2H),2.11 (td, J = 12.2, 7.1 Hz, 1H), 2.01-1.85 (m, 2H), 1.65 (dq, J = 12.3,8.2 Hz, 1H), 1.17 (d, J = 6.1 Hz, 6H) 157 N-(imidazo[1,2- ¹H NMR (400MHz, methanol-d₄) δ ppm (APCI(+)) a]pyridin-6- 8.78 (s, 1H), 8.21 (d, J= 2.0 Hz, 1H), 8.03 m/e 487 ylmethyl)-2-[{[2- (d, J = 2.1 Hz, 1H), 7.99(d, J = 11.6 Hz, (M + H)⁺ (propan-2- 2H), 7.90 (d, J = 9.4 Hz, 1H), 4.65(d, J = yloxy)ethyl]carbam- 3.9 Hz, 2H), 4.24 (dd, J = 15.2, 7.6 Hz,1H), oyl}(tetrahydrofuran- 4.12 (dd, J = 15.1, 8.0 Hz, 1H), 3.94 (td, J= 3-ylmethyl)amino]- 8.1, 5.7 Hz, 1H), 3.79-3.67 (m, 2H), 3.631,3-thiazole-5- (dt, J = 8.2, 4.7 Hz, 2H), 3.57 (t, J = 5.8 Hz,carboxamide 2H), 3.51-3.41 (m, 2H), 2.89-2.76 (m, 1H), 2.00 (td, J =13.3, 7.9 Hz, 1H), 1.73 (dt, J = 20.3, 6.4 Hz, 1H), 1.15 (d, J = 6.1 Hz,6H)

Example 116N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[2-oxo-4-(tetrahydrofuran-3-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamideExample 116A2-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and2-bromothiazole-5-carboxylic acid for 4-nitrobenzoic acid.

Example 116BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[2-oxo-4-(tetrahydrofuran-3-yl)-1,3-oxazolidin-3-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 53B, substituting4-(tetrahydrofuran-3-yl)oxazolidin-2-one for 4-cyanobenzylamine and2-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)thiazole-5-carboxamide for2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide. ¹H NMR(400 MHz, methanol-d₄) δ 8.79 (s, 1H), 8.22 (d, J=1.9 Hz, 1H), 8.03 (s,2H), 8.01-7.97 (m, 1H), 7.91 (d, J=9.5 Hz, 1H), 4.98-4.92 (m, 1H), 4.64(dt, J=8.6, 4.5 Hz, 3H), 4.57-4.49 (m, 1H), 3.97 (td, J=8.5, 3.9 Hz,1H), 3.81-3.71 (m, 1H), 3.71-3.59 (m, 2H), 2.26-2.02 (m, 1H), 1.96-1.85(m, 1H), 1.78-1.65 (m, 1H); (APCI(+)) m/e 414 (M+H)⁺.

TABLE 9 The following Examples were prepared essentially as described inExample 116, substituting the appropriate amine in Example 116A and theappropriate amine in Example 116B. Ex Name ¹H NMR MS 122 N-(imidazo[1,2-(ESI(+)) a]pyridin-6-ylmethyl)-2- m/e 420 (2-oxo-5-phenyl-1,3- (M + H)⁺oxazolidin-3-yl)-1,3- thiazole-5-carboxamide 158 2-[5-(4-chlorophenyl)-(ESI(+)) 2-oxo-1,3-oxazolidin-3- m/e 454 yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-6-ylmethyl)- 1,3-thiazole-5- carboxamide 181 N-(imidazo[1,2-¹H NMR (400 MHz, methanol-d₄) δ (APCI(+)) a]pyridin-7-ylmethyl)-2- ppm8.39 (d, J = 7.0 Hz, 1H), 8.04 (s, m/e 386 [(4R)-2-oxo-4-(propan- 1H),7.80 (s, 1H), 7.53 (s, 1H), 7.45 (s, (M + H)⁺ 2-yl)-1,3-oxazolidin-3-1H), 6.97-6.87 (m, 1H), 4.75 (dt, J = yl]-1,3-thiazole-5- 7.7, 3.8 Hz,1H), 4.52 (dd, J = 9.5, 6.3 carboxamide Hz, 2H), 2.85-2.65 (m, 1H), 0.99(d, J = 7.1 Hz, 3H), 0.84 (d, J = 6.9 Hz, 3H) 185 N-(imidazo[1,2- ¹H NMR(400 MHz, methanol-d₄) δ (APCI(+)) a]pyridin-7-ylmethyl)-2- ppm 9.26 (t,J = 5.5 Hz, 1H), 8.75 (d, J = m/e 386 [(4S)-2-oxo-4-(propan- 7.0 Hz,1H), 8.18 (d, J = 2.1 Hz, 1H), (M + H)⁺ 2-yl)-1,3-oxazolidin-3- 8.07 (s,1H), 8.00 (d, J = 2.1 Hz, 1H), yl]-1,3-thiazole-5- 7.81 (s, 1H), 7.48(d, J = 7.0 Hz, 1H), carboxamide 4.77 (dd, J = 7.7, 3.9 Hz, 1H), 4.55(dd, J = 10.7, 6.3 Hz, 2H), 2.76 (qd, J = 10.6, 7.1 Hz, 1H), 1.00 (d, J= 7.1 Hz, 3H), 0.84 (d, J = 6.9 Hz, 3H) 187 2-{(4R)-4- ¹H NMR (400 MHz,methanol-d₄) δ (APCI(+)) [(benzyloxy)methyl]-2- ppm 8.40 (d, J = 7.0 Hz,1H), 7.91 (s, m/e 464 oxo-1,3-oxazolidin-3- 1H), 7.80 (s, 1H), 7.53 (s,1H), 7.46 (s, (M + H)⁺ yl}-N-(imidazo[1,2- 1H), 7.20 (ddd, J = 15.4,11.1, 5.1 Hz, a]pyridin-7-ylmethyl)- 5H), 6.93 (dd, J = 7.0, 1.3 Hz,1H), 4.85 1,3-thiazole-5- (dd, J = 6.1, 2.6 Hz, 1H), 4.67-4.52carboxamide (m, 5H), 4.41 (d, J = 12.2 Hz, 1H), 4.12 (dd, J = 10.2, 3.2Hz, 1H), 3.63 (dd, J = 10.2, 1.6 Hz, 1H) 188 2-{(4S)-4- ¹H NMR (400 MHz,methanol-d₄) δ (APCI(+)) [(benzyloxy)methyl]-2- ppm 8.35 (d, J = 7.0 Hz,1H), 7.87 (s, m/e 464 oxo-1,3-oxazolidin-3- 1H), 7.75 (s, 1H), 7.48 (s,1H), 7.42 (s, (M + H)⁺ yl}-N-(imidazo[1,2- 1H), 7.16 (ddd, J = 19.3,11.3, 5.0 Hz, a]pyridin-7-ylmethyl)- 5H), 6.88 (dd, J = 7.0, 1.3 Hz,1H), 4.83- 1,3-thiazole-5- 4.75 (m, 1H), 4.62-4.47 (m, 5H), carboxamide4.36 (d, J = 12.2 Hz, 1H), 4.07 (dd, J = 10.2, 3.2 Hz, 1H), 3.59 (dd, J= 10.2, 1.6 Hz, 1H) 218 2-{5- ¹H NMR (400 MHz, methanol-d₄) δ (APCI(+))[(benzyloxy)methyl]-2- ppm 8.39 (d, J = 7.0 Hz, 1H), 8.03 (s, m/e 464oxo-1,3-oxazolidin-3- 1H), 7.79 (s, 1H), 7.53 (s, 1H), 7.45 (s, (M + H)⁺yl}-N-(imidazo[1,2- 1H), 7.36-7.18 (m, 5H), 6.92 (d, J =a]pyridin-7-ylmethyl)- 5.6 Hz, 1H), 5.02-4.99 (m, 2H), 4.591,3-thiazole-5- (d, J = 2.3 Hz, 6H), 3.76 (ddd, J = 14.8, carboxamide11.2, 3.2 Hz, 1H) 244 2-[(2S)-2- ¹H NMR (400 MHz, methanol-d₄) δ(APCI(+)) (hydroxymethyl)-5- ppm 9.25 (t, J = 5.7 Hz, 1H), 8.75 (d, J =m/e 372 oxopyrrolidin-1-yl]-N- 7.0 Hz, 1H), 8.18 (d, J = 1.9 Hz, 1H),(M + H)⁺ (imidazo[1,2-a]pyridin- 8.10 (s, 1H), 8.00 (d, J= 2.1 Hz, 1H),7-ylmethyl)-1,3- 7.81 (s, 1H), 7.48 (dd, J = 7.1, 1.3 Hz,thiazole-5-carboxamide 1H), 4.75-4.69 (m, 3H), 4.17 (dd, J = 11.7, 3.4Hz, 1H), 3.75 (dd, J = 11.7, 2.2 Hz, 1H), 2.88 (dt, J = 17.8, 10.1 Hz,1H), 2.57 (ddd, J = 17.7, 10.1, 2.3 Hz, 1H), 2.48-2.33 (m, 1H),2.33-2.18 (m, 1H) 245 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ(APCI(+)) a]pyridin-7-ylmethyl)-2- ppm 8.75 (d, J = 7.0 Hz, 1H), 8.18(d, J = m/e 358 [(4R)-4-methyl-2-oxo- 2.0 Hz, 1H), 8.07 (s, 1H), 8.00(t, J = (M + H)⁺ 1,3-oxazolidin-3-yl]- 2.4 Hz, 1H), 7.81 (s, 1H), 7.48(dd, J = 1,3-thiazole-5- 7.0, 1.4 Hz, 1H), 4.87-4.78 (m, 1H),carboxamide 4.73 (s, 2H), 4.69 (t, J = 8.5 Hz, 1H), 4.25 (dd, J = 8.7,3.9 Hz, 1H), 1.57 (d, J = 6.3 Hz, 3H) 249 N-(imidazo[1,2- ¹H NMR (400MHz, methanol-d₄) δ (APCI(+)) a]pyridin-7-ylmethyl)-2- ppm 9.26 (t, J =5.9 Hz, 1H), 8.75 (d, J = m/e 416 {2-oxo-5-[(propan-2- 7.0 Hz, 1H), 8.18(d, J = 2.0 Hz, 1H), (M + H)⁺ yloxy)methyl]-1,3- 8.06 (s, 1H), 8.00 (d,J = 2.1 Hz, 1H), oxazolidin-3-yl}-1,3- 7.81 (s, 1H), 7.48 (d, J = 7.0Hz, 1H), thiazole-5-carboxamide 4.98 (ddd, J = 9.1, 5.8, 2.9 Hz, 1H),4.73 (s, 2H), 4.31 (t, J = 9.5 Hz, 1H), 4.14 (dd, J = 9.9, 5.6 Hz, 1H),3.78 (dd, J = 11.2, 2.9 Hz, 1H), 3.73-3.60 (m, 2H), 1.13 (d, J = 6.1 Hz,6H) 251 2-[5-(hydroxymethyl)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm (APCI(+))2-oxo-1,3-oxazolidin-3- 9.17 (t, J = 6.2 Hz, 1H), 8.50 (d, J = 6.9 m/e374 yl]-N-(imidazo[1,2- Hz, 1H), 8.14 (s, 1H), 7.90 (s, 1H), 7.53 (M +H)⁺ a]pyridin-7-ylmethyl)- (s, 1H), 7.41 (s, 1H), 6.85 (d, J = 6.91,3-thiazole-5- Hz, 1H), 5.29 (t, J = 5.6 Hz, 1H), 4.93- carboxamide4.84 (m, 1H), 4.47 (d, J = 5.8 Hz, 2H), 4.24 (t, J = 9.4 Hz, 1H), 4.00(dd, J = 9.8, 5.8 Hz, 1H), 3.76-3.66 (m, 1H), 3.66-3.56 (m, 1H) 255N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ (APCI(+))a]pyridin-7-ylmethyl)-2- 8.40 (d, J = 7.0 Hz, 1H), 8.04 (s, 1H), m/e 416{(5S)-2-oxo-5-[(propan- 7.80 (s, 1H), 7.53 (s, 1H), 7.45 (s, 1H), (M +H)⁺ 2-yloxy)methyl]-1,3- 6.92 (d, J = 6.3 Hz, 1H), 5.01-4.94 (m,oxazolidin-3-yl}-1,3- 1H), 4.59 (s, 2H), 4.31 (t, J = 9.5 Hz,thiazole-5-carboxamide 1H), 4.13 (dd, J = 9.9, 5.6 Hz, 1H), 3.77 (dd, J= 11.2, 3.0 Hz, 1H), 3.72-3.58 (m, 2H), 1.13 (d, J = 6.1 Hz, 6H) 256N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ (APCI(+))a]pyridin-7-ylmethyl)-2- ppm 8.40 (d, J = 7.0 Hz, 1H), 8.04 (s, m/e 416{(5R)-2-oxo-5-[(propan- 1H), 7.80 (s, 1H), 7.53 (s, 1H), 7.45 (s, (M +H)⁺ 2-yloxy)methyl]-1,3- 1H), 6.92 (d, J = 7.0 Hz, 1H), 5.03-oxazolidin-3-yl}-1,3- 4.95 (m, 1H), 4.59 (s, 2H), 4.31 (t, J =thiazole-5-carboxamide 9.5 Hz, 1H), 4.13 (dd, J = 9.9, 5.7 Hz, 1H), 3.77(dd, J = 11.2, 3.0 Hz, 1H), 3.71-3.58 (m, 2H), 1.13 (d, J = 6.1 Hz, 6H)

Example 1174-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(2-cyclopentylacetamido)benzoic acid for 4-nitrobenzoic acid. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 10.09 (s, 1H), 9.00-8.93 (m, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.90-7.82 (m, 3H), 7.71-7.65 (m, 2H), 7.51 (d, J=1.2Hz, 1H), 7.40-7.35 (m, 1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 4.49 (d, J=5.9Hz, 2H), 2.37-2.31 (m, 2H), 2.31-2.16 (m, 1H), 1.81-1.68 (m, 2H),1.67-1.44 (m, 4H), 1.26-1.10 (m, 2H); MS (ESI(+)) m/e 377 (M+H)⁺.

Example 1182-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamideExample 118A 2-cyclopentyl-N-(4-nitrophenyl)acetamide

The title compound was prepared as described in Example 1A, substituting4-nitroaniline for 3-methylbutan-1-amine and 2-cyclopentylacetic acidfor 4-nitrobenzoic acid.

Example 118B N-(4-aminophenyl)-2-cyclopentylacetamide

The title compound was prepared as described in Example 1B, substituting2-cyclopentyl-N-(4-nitrophenyl)acetamide forN-isopentyl-4-nitrobenzamide.

Example 118C2-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide

The title compound was prepared as described in Example 1C, substitutingN-(4-aminophenyl)-2-cyclopentylacetamide for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (400 MHz, methanol-d₄) δ ppm8.76-8.69 (m, 1H), 8.16 (dd, J=2.2, 0.8 Hz, 1H), 7.98 (d, J=2.2 Hz, 1H),7.81-7.77 (m, 1H), 7.49-7.41 (m, 3H), 7.36-7.30 (m, 2H), 4.59 (s, 2H),2.37-2.24 (m, 3H), 1.90-1.77 (m, 2H), 1.75-1.52 (m, 4H), 1.32-1.18 (m,2H); MS (ESI(+)) m/e 392 (M+H)⁺.

Example 119N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide

The title compound was prepared as described in Example 51A,substituting 4-bromo-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.18 (t, J=5.7 Hz, 1H),8.75 (s, 1H), 8.28 (s, 2H), 8.02 (d, J=1.5 Hz, 1H), 7.97 (s, 1H), 7.89(d, J=8.5 Hz, 2H), 7.83-7.88 (m, 1H), 7.74-7.80 (m, 1H), 7.69 (d, J=8.3Hz, 2H), 4.56 (d, J=5.7 Hz, 2H), 3.92 (d, J=7.2 Hz, 2H), 2.13 (dq,J=13.6, 6.8 Hz, 1H), 0.85 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 374 (M+H)⁺.

Example 137N-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutanoyl)amino]-1,3-thiazole-5-carboxamideExample 137A 2-(3-methylbutanamido)thiazole-5-carboxylic acid

The title compound was prepared as described in Example 52A,substituting 3-methylbutanoyl chloride for 2-cyclopentylacetyl chlorideand methyl 2-aminothiazole-5-carboxylate for methyl 4-aminobenzoate.

Example 137BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-2-[(3-methylbutanoyl)amino]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and2-(3-methylbutanamido)thiazole-5-carboxylic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 12.31 (s, 1H), 9.05 (t, J=5.7 Hz,1H), 8.54 (s, 1H), 7.97-8.11 (m, 2H), 7.56-7.71 (m, 2H), 7.34 (d, J=9.2Hz, 1H), 4.44 (d, J=5.7 Hz, 2H), 2.33 (d, J=7.2 Hz, 2H), 2.07 (dq,J=13.6, 6.7, 6.6 Hz, 1H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 358(M+H)⁺.

Example 159N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamideExample 159A tert-butyl4-(4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)phenoxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yloxy)benzoic acid for4-nitrobenzoic acid.

Example 159BN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(piperidin-4-yloxy)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)phenoxy)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 159CN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(piperidin-4-yloxy)benzamide for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.79-8.74 (m, 1H), 8.23-8.19 (m, 1H),8.04-7.97 (m, 2H), 7.94-7.81 (m, 3H), 7.09-7.03 (m, 2H), 4.81-4.72 (m,1H), 4.69 (s, 2H), 3.91-3.77 (m, 2H), 3.62-3.48 (m, 2H), 3.04-2.92 (m,1H), 2.12-1.86 (m, 2H), 1.87-1.61 (m, 2H), 1.11 (d, J=6.7 Hz, 6H); MS(ESI(+)) m/e 421 (M+H)⁺.

TABLE 10 The following Examples were prepared essentially as describedin Example 159, substituting the appropriate amine in Example 159A andthe appropriate carboxylic acid in Example 159C. Ex Name ¹H NMR MS 1604-[(1- ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.80- (ESI(+))acetylpiperidin-4- 8.75 (m, 1H), 8.21 (dd, J = 2.2, 0.7 Hz, 1H), m/e 393yl)oxy]-N- 8.04-7.97 (m, 2H), 7.94-7.79 (m, 3H), 7.09- (M + H)⁺(imidazo[1,2- 7.03 (m, 2H), 4.78-4.70 (m, 1H), 4.69 (s, 2H),a]pyridin-6- 3.88-3.69 (m, 2H), 3.59-3.45 (m, 2H), 2.12ylmethyl)benzamide (s, 3H), 2.09-1.91 (m, 2H), 1.86-1.63 (m, 2H) 1614-{[1- ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.79- (ESI(+))(cyclopropylcar- 8.75 (m, 1H), 8.21 (dd, J = 2.2, 0.7 Hz, 1H), m/e 419bonyl)piperidin-4- 8.04-7.97 (m, 2H), 7.93-7.82 (m, 3H), 7.10- (M + H)⁺yl]oxy}-N- 7.04 (m, 2H), 4.81-4.73 (m, 1H), 4.69 (s, 2H), (imidazo[1,2-4.07-3.97 (m, 1H), 3.92-3.81 (m, 1H), 3.78- a]pyridin-6- 3.67 (m, 1H),3.57-3.48 (m, 1H), 2.13-1.92 ylmethyl)benzamide (m, 3H), 1.88-1.65 (m,2H), 0.91-0.78 (m, 4H) 162 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄)δ ppm 8.77 (ESI(+)) a]pyridin-6- (m, 1H), 8.23-8.19 (m, 1H), 8.04-7.97(m, m/e 463 ylmethyl)-4-{[1- 2H), 7.94-7.82 (m, 3H), 7.09-7.03 (m, 2H),(M + H)⁺ (tetrahydro-2H- 4.75 (m, 1H), 4.69 (s, 2H), 4.00-3.88 (m, 2H),pyran-4- 3.89-3.80 (m, 2H), 3.63-3.45 (m, 4H), 3.04-ylcarbonyl)piperidin-4- 2.93 (m, 1H), 2.11-1.92 (m, 2H), 1.86-1.65yl]oxy}benzamide (m, 4H), 1.66-1.58 (m, 2H) 163 4-{[1-(1,4-dioxan- ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.79- (ESI(+)) 2- 8.75 (m, 1H),8.23-8.19 (m, 1H), 8.04-7.97 m/e 465 ylcarbonyl)piperidin- (m, 2H),7.93-7.82 (m, 3H), 7.09-7.02 (m, (M + H)⁺ 4-yl]oxy}-N- 2H), 4.79-4.71(m, 1H), 4.69 (s, 2H), 4.47- (imidazo[1,2- 4.39 (m, 1H), 3.99-3.57 (m,9H), 3.56-3.37 a]pyridin-6- (m, 1H), 2.11-1.88 (m, 2H), 1.90-1.62 (m,ylmethyl)benzamide 2H) 164 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄)δ ppm 8.79- (ESI(+)) a]pyridin-6- 8.76 (m, 1H), 8.23-8.19 (m, 1H),8.04-7.97 m/e 449 ylmethyl)-4-({1- (m, 2H), 7.94-7.82 (m, 3H), 7.09-7.03(m, (M + H)⁺ [(2S)- 2H), 4.79-4.71 (m, 2H), 4.69 (s, 2H), 3.98-tetrahydrofuran-2- 3.72 (m, 4H), 3.66-3.43 (m, 2H), 2.26-2.13ylcarbonyl]piperidin-4- (m, 1H), 2.13-1.86 (m, 5H), 1.88-1.65 (m,yl}oxy)benzamide 2H) 165 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δppm 8.79- (ESI(+)) a]pyridin-6- 8.75 (m, 1H), 8.23-8.19 (m, 1H),8.04-7.97 m/e 449 ylmethyl)-4-({1- (m, 2H), 7.93-7.82 (m, 3H), 7.09-7.03(m, (M + H)⁺ [(2R)- 2H), 4.79-4.71 (m, 1H), 4.69 (s, 1H), 4.00-tetrahydrofuran-2- 3.71 (m, 4H), 3.67-3.43 (m, 1H), 2.26-2.13ylcarbonyl]piperidin-4- (m, 1H), 2.13-1.86 (m, 5H), 1.88-1.65 (m,yl}oxy)benzamide 2H) 166 4-{[1-(2-hydroxy- ¹H NMR (400 MHz, methanol-d₄)δ ppm 8.79- (ESI(+)) 2-methylpropanoyl)pi- 8.75 (m, 1H), 8.21 (dd, J =2.2, 0.7 Hz, 1H), m/e 437 peridin-4- 8.04-7.97 (m, 2H), 7.93-7.81 (m,3H), 7.08- (M + H)⁺ yl]oxy}-N- 7.02 (m, 2H), 4.78-4.70 (m, 1H), 4.69 (s,2H), (imidazo[1,2- 4.41-3.50 (m, 4H), 2.10-1.95 (m, 2H), 1.82-a]pyridin-6- 1.69 (m, 2H), 1.44 (s, 6H) ylmethyl)benzamide 167N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.79- (ESI(+))a]pyridin-6- 8.75 (m, 1H), 8.21 (dd, J = 2.2, 0.7 Hz, 1H), m/e 451ylmethyl)-4-({1- 8.04-7.97 (m, 2H), 7.93-7.82 (m, 3H), 7.09- (M + H)⁺[(propan-2- 7.03 (m, 2H), 4.80-4.72 (m, 1H), 4.69 (s, 2H),yloxy)acetyl]piper- 4.19 (s, 2H), 3.87-3.73 (m, 2H), 3.73-3.62 idin-4-(m, 1H), 3.59-3.45 (m, 2H), 2.11-1.93 (m, yl}oxy)benzamide 2H),1.87-1.68 (m, 2H), 1.19 (d, J = 6.1 Hz, 6H) 168 4-[(1- ¹H NMR (400 MHz,methanol-d₄) δ ppm 8.79- (ESI(+)) butanoylpiperidin- 8.75 (m, 1H), 8.21(dd, J = 2.2, 0.7 Hz, 1H), m/e 421 4-yl)oxy]-N- 8.04-7.97 (m, 2H),7.96-7.81 (m, 3H), 7.08- (M + H)⁺ (imidazo[1,2- 7.02 (m, 2H), 4.78-4.70(m, 1H), 4.69 (s, 2H), a]pyridin-6- 3.90-3.73 (m, 2H), 3.59-3.46 (m,2H), 2.40 ylmethyl)benzamide (t, J = 7.5 Hz, 2H), 2.10-1.90 (m, 2H),1.84- 1.57 (m, 4H), 0.98 (t, J = 7.4 Hz, 3H) 169 N-(imidazo[1,2- ¹H NMR(400 MHz, methanol-d₄) δ ppm 8.80- (ESI(+)) a]pyridin-6- 8.75 (m, 1H),8.21 (dd, J = 2.2, 0.7 Hz, 1H), m/e 451 ylmethyl)-4-{[1- 8.04-7.97 (m,2H), 7.94-7.82 (m, 3H), 7.09- (M + H)⁺ (3-methoxy-2- 7.03 (m, 2H),4.80-4.71 (m, 1H), 4.69 (s, 2H), methylpropanoyl) 4.01-3.71 (m, 2H),3.71-3.41 (m, 3H), 3.38- piperidin-4- 3.31 (m, 1H), 3.30 (s, 3H),3.26-3.16 (m, 1H), yl]oxy}benzamide 2.12-1.88 (m, 2H), 1.87-1.61 (m,2H), 1.06 (d, J = 6.8 Hz, 3H) 170 N-(imidazo[1,2- ¹H NMR (400 MHz,methanol-d₄) δ ppm 8.79- (ESI(+)) a]pyridin-6- 8.75 (m, 1H), 8.21 (dd, J= 2.2, 0.7 Hz, 1H), m/e 461 ylmethyl)-4-{[1- 8.04-7.97 (m, 2H),7.94-7.81 (m, 3H), 7.09- (M + H)⁺ (3,3,3- 7.03 (m, 2H), 4.80-4.73 (m,1H), 4.69 (s, 2H), trifluoropropanoyl)pi- 3.90-3.72 (m, 2H), 3.66-3.47(m, 4H), 2.11- peridin-4- 1.90 (m, 2H), 1.91-1.68 (m, 2H)yl]oxy}benzamide 171 N-(imidazo[1,2- ¹H NMR (400 MHz, methanol-d₄) δ ppm8.79- (ESI(+)) a]pyridin-6- 8.76 (m, 1H), 8.21 (dd, J = 2.1, 0.7 Hz,1H), m/e 477 ylmethyl)-4-{[1- 8.04-7.97 (m, 2H), 7.93-7.82 (m, 3H),7.09- (M + H)⁺ (tetrahydro-2H- 7.03 (m, 2H), 4.78-4.71 (m, 1H), 4.68 (s,2H), pyran-4- 3.97-3.74 (m, 4H), 3.59-3.48 (m, 2H), 3.48-ylacetyl)piperidin- 3.38 (m, 2H), 2.37 (d, J = 7.0 Hz, 2H), 2.10- 4-1.90 (m, 3H), 1.85-1.60 (m, 4H), 1.41-1.26 yl]oxy}benzamide (m, 2H) 1724-{[1- ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.79- (ESI(+))(cyclopropylace- 8.75 (m, 1H), 8.21 (dd, J = 2.2, 0.7 Hz, 1H), m/e 433tyl)piperidin-4- 8.04-7.97 (m, 2H), 7.93-7.82 (m, 3H), 7.09- (M + H)⁺yl]oxy}-N- 7.03 (m, 2H), 4.79-4.71 (m, 1H), 4.69 (s, 2H), (imidazo[1,2-3.92-3.73 (m, 2H), 3.60-3.47 (m, 2H), 2.36 a]pyridin-6- (d, J = 6.8 Hz,2H), 2.10-1.91 (m, 2H), 1.86- ylmethyl)benzamide 1.65 (m, 2H), 1.08-0.94(m, 1H), 0.58-0.47 (m, 2H), 0.23-0.16 (m, 2H) 173 N-(imidazo[1,2- ¹H NMR(400 MHz, methanol-d₄) δ ppm 8.80- (ESI(+)) a]pyridin-6- 8.75 (m, 1H),8.22-8.19 (m, 1H), 8.04-7.97 m/e 463 ylmethyl)-4-{[1- (m, 2H), 7.92-7.81(m, 3H), 7.09-7.03 (m, (M + H)⁺ (tetrahydrofuran- 2H), 4.79-4.70 (m,1H), 4.69 (s, 2H), 4.29- 2- 4.18 (m, 1H), 3.94-3.66 (m, 4H), 3.65-3.45ylacetyl)piperidin- (m, 2H), 2.76 (dd, J = 14.8, 7.6 Hz, 1H), 2.52 4-(dd, J = 14.8, 5.2 Hz, 1H), 2.18-1.67 (m, 7H), yl]oxy}benzamide1.69-1.53 (m, 1H) 411 4-[(1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.96 (t, J= (ESI(+)) acetylpiperidin-4- 5.9 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H),7.88 (m, m/e 393 yl)oxy]-N- 3H), 7.51 (s, 1H), 7.37 (s, 1H), 7.07 (m,2H), (M + H)⁺ (imidazo[1,2- 6.85 (dd, J = 6.9, 1.6 Hz, 1H), 4.72 (m,1H), a]pyridin-7- 4.49 (d, J = 5.9 Hz, 2H), 3.85 (m, 1H), 3.68 (m,ylmethyl)benzamide 1H), 3.50-3.15 (m, 2H), 2.02 (s, 3H), 2.03- 1.85 (m2H), 1.62 (m, 1H), 1.51 (m, 1H) 412 N-(imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.96 (t, J = (ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (dd,J = 6.9, 0.9 Hz, 1H), m/e 421 ylmethyl)-4-{[1- 7.88 (m, 3H), 7.51 (d, J= 1.2 Hz, 1H), 7.37 (s, (M + H)⁺ (2- 1H), 7.07 (m, 2H), 6.85 (dd, J =6.9, 1.7 Hz, methylpropanoyl) 1H), 4.73 (m, 1H), 4.49 (d, J = 5.9 Hz,2H), piperidin-4- 3.96-3.70 (m, 2H), 3.45-3.20 (m, 2H), 2.89yl]oxy}benzamide (m, 1H), 1.93 (m, 2H), 1.58 (m, 2H), 1.00 (d, J = 6.7Hz, 6H) 413 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.96 (t, J =(ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (dd, J = 6.9, 0.9 Hz, 1H), m/e435 ylmethyl)-4-({1- 7.88 (m, 3H), 7.51 (s, 1H), 7.37 (s, 1H), 7.07 (M +H)⁺ [(2S)-2- (m, 2H), 6.85 (dd, J = 6.9, 1.6 Hz, 1H), 4.74 (m,methylbutanoyl]pi- 1H), 4.49 (d, J = 5.9 Hz, 2H), 4.00-3.74 (m,peridin-4- 2H), 3.50-3.15 (m, 2H), 2.72 (m, 1H), 1.95 yl}oxy)benzamide(m, 2H), 1.54 (m, 3H), 1.27 (m, 1H), 0.98 (d, J = 6.7 Hz, 3H), 0.81 (t,J = 7.4 Hz, 3H) 414 4-{[1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.95 (t, J =(ESI(+)) (cyclopropylace- 5.9 Hz, 1H), 8.48 (dd, J = 6.9, 0.9 Hz, 1H),m/e 433 tyl)piperidin-4- 7.88 (m, 3H), 7.51 (d, J = 1.2 Hz, 1H), 7.37(s, (M + H)⁺ yl]oxy}-N- 1H), 7.07 (m, 2H), 6.85 (dd, J = 7.0, 1.7 Hz,(imidazo[1,2- 1H), 4.73 (m, 1H), 4.49 (d, J = 5.9 Hz, 2H), a]pyridin-7-3.89 (m, 1H), 3.69 (m, 1H), 3.40-3.15 (m, ylmethyl)benzamide 2H), 2.28(d, J = 6.7 Hz, 2H), 1.93 (m, 2H), 1.85-1.41 (m, 2H), 0.95 (m, 1H), 0.45(m, 2H), 0.12 (m, 2H) 415 4-[(1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.96(t, J = (ESI(+)) benzoylpiperidin- 5.9 Hz, 1H), 8.48 (dd, J = 6.9, 0.9Hz, 1H), m/e 455 4-yl)oxy]-N- 7.90 (m, 3H), 7.51 (m, 1H), 7.47-7.37 (m,(M + H)⁺ (imidazo[1,2- 5H), 7.36 (m, 1H), 7.07 (m, 2H), 6.84 (dd, J =a]pyridin-7- 7.0, 1.7 Hz, 1H), 4.78 (m, 1H), 4.49 (d, J = 5.9ylmethyl)benzamide Hz, 2H), 4.00 (m, 1H), 3.55 (m, 1H), 3.45- 3.15 (m,2H), 2.00 (m, 2H), 164 (m, 2H) 416 N-(imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.96 (t, J = (ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (dd,J = 6.9, 0.9 Hz, 1H), m/e 451 ylmethyl)-4-({1- 7.88 (m, 3H), 7.51 (d, J= 1.2 Hz, 1H), 7.37 (s, (M + H)⁺ [(propan-2- 1H), 7.07 (m, 2H), 6.85(dd, J = 7.0, 1.7 Hz, yloxy)acetyl]piper- 1H), 4.74 (m, 1H), 4.49 (d, J= 5.9 Hz, 2H), idin-4- 4.10 (d, J = 1.1 Hz, 2H), 3.85 (m, 1H), 3.70 (m,yl}oxy)benzamide 1H), 3.60 (m, 1H), 3.40-3.15 (m, 2H), 1.97 (m, 2H),1.69-1.45 (m, 2H), 1.11 (d, J = 6.1 Hz, 6H) 417 4-{[1-(2-hydroxy- ¹H NMR(400 MHz, DMSO-d₆) δ ppm 8.96 (t, J = (ESI(+)) 2- 5.9 Hz, 1H), 8.48 (dd,J = 6.9, 0.9 Hz, 1H), m/e 437 methylpropanoyl)pi- 7.88 (m, 3H), 7.51 (d,J = 1.2 Hz, 1H), 7.37 (s, (M + H)⁺ peridin-4- 1H), 7.07 (m, 2H), 6.85(dd, J = 7.0, 1.7 Hz, yl]oxy}-N- 1H), 5.42 (m, 1H), 4.73 (m, 1H), 4.49(d, J = (imidazo[1,2- 5.9 Hz, 2H), 4.42-3.78 (m, 2H), 3.70-3.20a]pyridin-7- (m, 2H), 1.95 (m, 2H), 1.57 (m, 2H), 1.32 (s,ylmethyl)benzamide 6H) 418 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δppm 8.96 (t, J = (ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (dd, J = 6.9,0.9 Hz, 1H), m/e 449 ylmethyl)-4-({1- 7.88 (m, 3H), 7.51 (d, J = 1.2 Hz,1H), 7.37 (s, (M + H)⁺ [(2R)- 1H), 7.07 (m, 2H), 6.85 (dd, J = 7.0, 1.7Hz, tetrahydrofuran-2- 1H), 4.79-4.64 (m, 2H), 4.49 (d, J = 5.9 Hz,ylcarbonyl]piper- 2H), 3.95-3.70 (m, 4H), 3.50-3.15 (m, 2H), idin-4-2.10-1.90 (m, 4H), 1.90-1.75 (m, 2H), 1.70- yl}oxy)benzamide 1.43 (m,2H) 419 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.96 (t, J =(ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (dd, J = 6.9, 0.9 Hz, 1H), m/e449 ylmethyl)-4-({1- 7.88 (m, 3H), 7.51 (d, J = 1.2 Hz, 1H), 7.37 (s,(M + H)⁺ [(2S)- 1H), 7.07 (m, 2H), 6.85 (dd, J = 6.9, 1.7 Hz,tetrahydrofuran-2- 1H), 4.79-4.64 (m, 2H), 4.49 (d, J = 5.9 Hz,ylcarbonyl]piper- 2H), 3.94-3.67 (m, 4H), 3.50-3.15 (m, 2H), idin-4-2.10-1.90 (m, 4H), 1.90-1.75 (m, 2H), 1.70- yl}oxy)benzamide 1.43 (m,2H) 420 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.96 (t, J =(ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (dd, J = 6.9, 0.9 Hz, 1H), m/e463 ylmethyl)-4-{[1- 7.88 (m, 3H), 7.51 (d, J = 1.2 Hz, 1H), 7.37 (s,(M + H)⁺ (tetrahydro-2H- 1H), 7.07 (m, 2H), 6.85 (dd, J = 7.0, 1.7 Hz,pyran-4- 1H), 4.73 (m, 1H), 4.49 (d, J = 5.9 Hz, 2H), ylcarbonyl)piper-3.84 (m, 4H), 3.45-3.15 (m, 4H), 2.90 (m, idin-4- 1H), 1.96 (m, 2H),1.65-1.45 (m, 6H) yl]oxy}benzamide 421 4-{[1-(1,4-dioxan- ¹H NMR (400MHz, DMSO-d₆) δ ppm 8.96 (t, J = (ESI(+)) 2- 6.0 Hz, 1H), 8.48 (dd, J =6.9, 0.9 Hz, 1H), m/e 465 ylcarbonyl)piper- 7.89 (m, 3H), 7.51 (d, J =1.2 Hz, 1H), 7.37 (d, (M + H)⁺ idin-4-yl]oxy}-N- J = 1.5 Hz, 1H), 7.07(m, 2H), 6.85 (dd, J = 7.0, (imidazo[1,2- 1.7 Hz, 1H), 4.74 (m, 1H),4.49 (d, J = 5.9 Hz, a]pyridin-7- 2H), 4.35 (dd, J = 9.4, 2.8 Hz, 1H),3.90-3.55 ylmethyl)benzamide (m, 7H), 3.55-3.15 (m, 3H), 1.98 (m, 2H),1.75-1.40 (m, 2H) 422 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm8.95 (t, J = (ESI(+)) a]pyridin-7- 5.9 Hz, 1H), 8.48 (d, J = 7.0 Hz,1H), 7.89 (m, m/e 477 ylmethyl)-4-{[1- 3H), 7.51 (s, 1H), 7.37 (bs, 1H),7.07 (m, 2H), (M + H)⁺ (tetrahydro-2H- 6.85 (dd, J = 6.9, 1.7 Hz, 1H),4.72 (m, 1H), pyran-4- 4.49 (d, J = 5.9 Hz, 2H), 3.95-3.67 (m, 4H),ylacetyl)piperidin- 3.45-3.15 (m, 5H), 2.28 (m, 2H), 1.93 (m, 4- 2H),1.67-1.42 (m, 4H), 1.26-1.12 (m, 2H) yl]oxy}benzamide 423N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.96 (t, J = (ESI(+))a]pyridin-7- 5.9 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.89 (m, m/e 478ylmethyl)-4-{[1- 3H), 7.51 (s, 1H), 7.37 (s, 1H), 7.07 (m, 2H), (M + H)⁺(morpholin-4- 6.85 (dd, J = 7.0, 1.6 Hz, 1H), 4.73 (m, 1H),ylacetyl)piperidin- 4.49 (d, J = 5.8 Hz, 2H), 3.86 (m, 2H), 3.57 (m, 4-4H), 3.50-3.20 (m, 2H), 3.20-3.05 (m, 2H), yl]oxy}benzamide 2.40 (m,4H), 2.08-1.89 (m, 2H), 1.70-1.41 (m, 2H)

Example 2042-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamideExample 204A2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and2-bromothiazole-5-carboxylic acid for 4-nitrobenzoic acid.

Example 204B2-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 51A,substituting2-methyl-1-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrrol-1-yl)propan-2-olfor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamidefor 4-bromoaniline. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.41 (d, J=7.05Hz, 1H) 8.27 (d, J=7.92 Hz, 2H) 8.00 (s, 1H) 7.80 (s, 1H) 7.53 (s, 1H)7.47 (s, 1H) 6.93 (dd, J=6.99, 1.36 Hz, 1H) 4.61 (s, 2H) 4.16 (s, 2H)1.20 (s, 6H); MS (ESI)(+)) m/e 397 (M+H)⁺.

Example 205N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 51A,substituting2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamide for4-bromoaniline. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.40 (d, J=6.94 Hz,1H) 8.27 (d, J=7.48 Hz, 2H) 8.00 (s, 1H) 7.80 (s, 1H) 7.53 (s, 1H) 7.47(s, 1H) 6.93 (d, J=6.83 Hz, 1H) 4.61 (s, 2H) 4.01 (d, J=7.26 Hz, 2H)2.12-2.30 (m, 1H) 0.93 (d, J=6.61 Hz, 6H); MS (ESI)(+)) m/e 381 (M+H)⁺.

Example 207 tert-butyl{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(tert-butoxycarbonylamino)benzoic acid for 4-nitrobenzoic acid. ¹H NMR(300 MHz, DMSO-d₆) δ ppm 9.62 (s, 1H), 8.92 (t, J=6.0 Hz, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.90-7.79 (m, 3H), 7.57-7.49 (m, 3H), 7.39-7.35 (m,1H), 6.85 (dd, J=7.0, 1.6 Hz, 1H), 4.48 (d, J=5.8 Hz, 2H), 1.49 (s, 9H);MS (ESI(+)) m/e 367 (M+H)⁺.

Example 208N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamideExample 208A tert-butyl{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(tert-butoxycarbonylamino)benzoic acid for 4-nitrobenzoic acid.

Example 208B 4-amino-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate fortert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 208CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]benzamide

The title compound was prepared as described in Example 1A, substituting4-amino-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for3-methylbutan-1-amine and 2-(tetrahydro-2H-pyran-4-yl)acetic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.74 (dd,J=7.0, 0.9 Hz, 1H), 8.17 (dd, J=2.2, 0.7 Hz, 1H), 7.98 (d, J=2.2 Hz,1H), 7.91-7.84 (m, 2H), 7.81-7.78 (m, 1H), 7.75-7.68 (m, 2H), 7.49 (dd,J=7.0, 1.6 Hz, 1H), 4.79-4.74 (m, 2H), 3.98-3.89 (m, 2H), 3.50-3.38 (m,2H), 2.38-2.32 (m, 2H), 2.20-2.02 (m, 1H), 1.74-1.61 (m, 2H), 1.47-1.28(m, 2H); MS (ESI(+)) m/e 393 (M+H)⁺.

TABLE 11 The following Examples were prepared essentially as describedin Example 208, substituting the appropriate carboxylic acid in Example208A and the appropriate carboxylic acid in Example 208C. Ex Name MS 209N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-2- (ESI(+))ylacetyl)amino]benzamide m/e 379 (M + H)⁺ 210N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[3-(tetrahydrofuran-2- (ESI(+))yl)propanoyl]amino}benzamide m/e 393 (M + H)⁺ 211N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(propan-2- (ESI(+))yloxy)acetyl]amino}benzamide m/e 367 (M + H)⁺ 2124-[(3-cyclopentylpropanoyl)amino]-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 391 (M + H)⁺ 213 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(4- (ESI(+))methylpentanoyl)amino]benzamide m/e 365 (M + H)⁺ 214N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(tetrahydrofuran-3- (ESI(+))ylacetyl)amino]benzamide m/e 379 (M + H)⁺ 3054-[(cyclopentylacetyl)amino]-3-fluoro-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 395 (M + H)⁺ 4634-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 395 (M + H)⁺ 867N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2- (ESI(+))methoxyphenyl)acetyl]amino}benzamide m/e 415 (M + H)⁺ 868N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4- (ESI(+))[(phenylacetyl)amino]benzamide m/e 385 (M + H)⁺ 8694-(benzoylamino)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide (ESI(+))m/e 371 (M + H)⁺ 870 2,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)carbamoyl]phenyl}benzamide m/e 407 (M + H)⁺ 8713,5-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)carbamoyl]phenyl}benzamide m/e 407 (M + H)⁺ 8723,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)carbamoyl]phenyl}benzamide m/e 407 (M + H)⁺ 8732,4-difluoro-N-{4-[(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)carbamoyl]phenyl}benzamide m/e 407 (M + H)⁺ 8742-fluoro-N-{4-[(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)carbamoyl]phenyl}benzamide m/e 389 (M + H)⁺ 875N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-3- (ESI(+))methoxybenzamide m/e 401 (M + H)⁺ 8764-{[(2-fluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 403 (M + H)⁺ 880N-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-2- (ESI(+))methoxybenzamide m/e 401 (M + H)⁺ 8904-{[(2,5-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 421 (M + H)⁺ 8914-{[(2,4-difluorophenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 421 (M + H)⁺ 8954-{[difluoro(phenyl)acetyl]amino}-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 421 (M + H)⁺ 896N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[(2-methyl-2- (ESI(+))phenylpropanoyl)amino]benzamide m/e 413 (M + H)⁺

Example 2154-[(4-cyanobenzyl)(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamideExample 215A methyl 4-(4-cyanobenzylamino)benzoate

A solution of methyl 4-aminobenzoate (0.2 g, 1.323 mmol) and4-formylbenzonitrile (0.177 g, 1.350 mmol) in methanol (2 ml) anddichloromethane (4 ml) was treated with acetic acid (0.379 ml, 6.62mmol) followed by MP-cyanoborohydride (1.151 g, 2.65 mmol) and thereaction was slowly stirred at room temperature. After 16 hours, themixture was filtered and concentrated and the concentrate waspartitioned between 2 N sodium hydroxide and dichloromethane. Theorganic phase was concentrated to give the title compound with 30% ofremaining 4-formylbenzonitrile.

Example 215B methyl 4-(N-(4-cyanobenzyl)-2-cyclopentylacetamido)benzoate

The title compound was prepared as described in Example 52A,substituting methyl 4-(4-cyanobenzylamino)benzoate for methyl4-aminobenzoate.

Example 215C 4-(N-(4-cyanobenzyl)-2-cyclopentylacetamido)benzoic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 4-(N-(4-cyanobenzyl)-2-cyclopentylacetamido)benzoate for methyl4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 215D4-[(4-cyanobenzyl)(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(N-(4-cyanobenzyl)-2-cyclopentylacetamido)benzoic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.08 (t, J=5.8 Hz,1H), 8.47 (s, 1H), 7.94 (s, 1H), 7.90-7.85 (m, 2H), 7.79-7.74 (m, 2H),7.56-7.49 (m, 2H), 7.43-7.37 (m, 2H), 7.36-7.30 (m, 2H), 7.21 (dd,J=9.3, 1.7 Hz, 1H), 4.98 (bs, 2H), 4.45 (d, J=5.8 Hz, 2H), 2.19-2.13 (m,3H), 1.74-1.66 (m, 2H), 1.51-1.38 (m, 4H), 1.01-0.92 (m, 2H); MS(ESI(+)) m/e 492 (M+H)⁺.

Example 216 tert-butyl4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.56(s, 1H), 8.51-8.45 (m, 1H), 7.88 (s, 1H), 7.52-7.49 (m, 1H), 7.39-7.36(m, 1H), 7.35-7.30 (m, 2H), 7.12-7.07 (m, 2H), 6.83 (dd, J=7.0, 1.6 Hz,1H), 6.67 (t, J=6.0 Hz, 1H), 4.32 (d, J=6.0 Hz, 2H), 4.10-4.00 (m, 2H),2.89-2.65 (m, 2H), 2.62-2.54 (m, 1H), 1.75-1.66 (m, 2H), 1.49-1.37 (m,11H); MS (ESI(+)) m/e 450 (M+H)⁺.

Example 217 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.02 (t, J=6.0 Hz, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.90-7.81 (m, 3H), 7.51 (d, J=1.2 Hz, 1H), 7.40-7.32(m, 3H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.13-4.03(m, 2H), 2.91-2.69 (m, 3H), 1.82-1.72 (m, 2H), 1.60-1.44 (m, 2H), 1.42(s, 9H); MS (ESI(+)) m/e 435 (M+H)⁺.

Example 2201-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}ureaExample 220A1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(piperidin-4-yl)phenyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 220B1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 1A, substituting1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(piperidin-4-yl)phenyl)ureafor 3-methylbutan-1-amine and tetrahydrofuran-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.72 (d, J=7.0Hz, 1H), 8.17-8.12 (m, 1H), 7.98-7.93 (m, 1H), 7.78 (bs, 1H), 7.48-7.41(m, 1H), 7.35-7.28 (m, 2H), 7.18-7.12 (m, 2H), 4.81-4.72 (m, 1H),4.67-4.55 (m, 3H), 4.19-4.08 (m, 1H), 4.01-3.91 (m, 1H), 3.90-3.81 (m,1H), 3.24-3.09 (m, 1H), 2.85-2.67 (m, 2H), 2.30-2.14 (m, 1H), 2.09-1.79(m, 5H), 1.73-1.46 (m, 2H); MS (ESI(+)) m/e 448 (M+H)⁺.

TABLE 12 The following Examples were prepared essentially as describedin Example 220, substituting the appropriate carboxylic acid in Example220B. Ex Name MS 2211-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-(ESI(+)) 4-ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 462 (M + H)⁺ 2221-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 464 (M + H)⁺ 2231-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-(ESI(+)) 4-ylacetyl)piperidin-4-yl]phenyl}urea m/e 476 (M + H)⁺ 2241-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(morpholin-4- (ESI(+))ylacetyl)piperidin-4-yl]phenyl}urea m/e 477 (M + H)⁺ 2251-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-(ESI(+)) ylacetyl)piperidin-4-yl]phenyl}urea m/e 462 (M + H)⁺ 2261-{4-[1-(3-hydroxy-3-methylbutanoyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 450 (M + H)⁺ 2271-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 436 (M + H)⁺ 2281-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2- (ESI(+))methylpropanoyl)piperidin-4-yl]phenyl}urea m/e 420 (M + H)⁺ 2291-[4-(1-benzoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)urea m/e 454 (M + H)⁺ 2431-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4- (ESI(+))yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7- m/e 510ylmethyl)urea (M + H)⁺ 2861-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3S)-tetrahydrofuran-(ESI(+)) 3-ylcarbonyl]piperidin-4-yl}phenyl)urea m/e 448 (M + H)⁺ 2871-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3R)- (ESI(+))tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)urea m/e 448 (M + H)⁺288 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-tetrahydrofuran-(ESI(+)) 2-ylcarbonyl]piperidin-4-yl}phenyl)urea m/e 448 (M + H)⁺ 2891-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2R)- (ESI(+))tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)urea m/e 448 (M + H)⁺709 1-[4-(1-butanoylpiperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)urea m/e 420 (M + H)⁺ 7101-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2S)-2- (ESI(+))methylbutanoyl]piperidin-4-yl}phenyl)urea m/e 434 (M + H)⁺ 7111-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2- (ESI(+))methylcyclopropyl)carbonyl]piperidin-4-yl}phenyl)urea m/e 432 (M + H)⁺712 1-{4-[1-(cyclopropylacetyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)urea m/e 432 (M + H)⁺ 7131-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3,3,3- (ESI(+))trifluoropropanoyl)piperidin-4-yl]phenyl}urea m/e 460 (M + H)⁺ 7141-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,4,4- (ESI(+))trifluorobutanoyl)piperidin-4-yl]phenyl}urea m/e 474 (M + H)⁺ 7151-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}phenyl)-3-(ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 496 (M + H)⁺ 7161-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1- (ESI(+))(phenylacetyl)piperidin-4-yl]phenyl}urea m/e 468 (M + H)⁺ 7191-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)urea m/e 472 (M + H)⁺ 7201-{4-[1-(3-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)urea m/e 472 (M + H)⁺ 7211-{4-[1-(4-fluorobenzoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)urea m/e 472 (M + H)⁺ 7221-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 490 (M + H)⁺ 7231-{4-[1-(3,4-difluorobenzoyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 490 (M + H)⁺ 7241-{4-[1-(3,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 490 (M + H)⁺ 7251-{4-[1-(2,5-difluorobenzoyl)piperidin-4-yl]phenyl}-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 490 (M + H)⁺ 9381-(4-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 489 (M + H)⁺ 9391-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(3-methylbut-2- ESI(+))enoyl)piperidin-4-yl]phenyl}urea m/e 432 (M + H)⁺ 9401-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 448 (M + H)⁺ 9411-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methylcyclopent-ESI(+)) 1-en-1-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 458 (M + H)⁺942 1-{4-[1-(2-ethylbutanoyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)urea m/e 448 (M + H)⁺ 9431-(4-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}phenyl)-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 502 (M + H)⁺ 9441-{4-[1-(2,4-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 514 (M + H)⁺ 9451-{4-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 458 (M + H)⁺ 9461-{4-[1-(2,5-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 514 (M + H)⁺ 9471-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2- ESI(+))methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea m/e 498 (M + H)⁺ 9481-{4-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 498 (M + H)⁺ 9491-{4-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 514 (M + H)⁺ 9501-{4-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 477 (M + H)⁺ 9511-(4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 503 (M + H)⁺ 9521-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3- ESI(+))methoxyphenyl)acetyl]piperidin-4-yl}phenyl)urea m/e 498 (M + H)⁺ 9531-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-oxo-2,3-dihydro-ESI(+)) 1H-inden-4-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 508 (M +H)⁺ 954 1-{4-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]phenyl}-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 513 (M + H)⁺ 9551-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-2-methylbut-2-ESI(+)) enoyl]piperidin-4-yl}phenyl)urea m/e 432 (M + H)⁺ 9561-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(1H-indol-3- ESI(+))ylacetyl)piperidin-4-yl]phenyl}urea m/e 507 (M + H)⁺ 9571-{4-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 484 (M + H)⁺ 10111-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(propan-2-yl)-1H-ESI(+)) pyrazol-3-yl]carbonyl}piperidin-4-yl)phenyl]urea m/e 486 (M +H)⁺ 10121-(4-{1-[(2S)-2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl]piperidin-ESI(+)) 4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512(M + H)⁺ 1013 1-(4-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5- ESI(+))yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7- m/e 497ylmethyl)urea (M + H)⁺ 10141-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-4,5,6,7- ESI(+))tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 512(M + H)⁺ 10151-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-ESI(+)) 2,1-benzoxazol-3-ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 499(M + H)⁺ 10161-(4-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 507 (M + H)⁺1017 1-(4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-ESI(+)) yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 487 (M +H)⁺ 1018 1-(4-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-ESI(+)) yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 507 (M +H)⁺ 10191-(4-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 489 (M + H)⁺ 10201-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[1-(pyridin-2- ESI(+))yl)cyclopropyl]carbonyl}piperidin-4-yl)phenyl]urea m/e 495 (M + H)⁺ 10211-(4-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512 (M + H)⁺1022 1-[4-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-ESI(+)) yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 494 (M +H)⁺ 1023 1-{4-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-ESI(+)) yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512 (M +H)⁺ 1024 1-{4-[1-(2,3-dihydro-1-benzofuran-2-ylcarbonyl)piperidin-4-ESI(+)) yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 496 (M +H)⁺ 1025 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4- ESI(+))methoxycyclohexyl)carbonyl]piperidin-4-yl}phenyl)urea m/e 490 (M + H)⁺1026 1-{4-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-ESI(+)) yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512 (M +H)⁺ 1027 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-4-ESI(+)) ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 505 (M + H)⁺ 10281-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-1,3- ESI(+))benzoxazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 509 (M + H)⁺1029 1-(4-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-ESI(+)) 4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 514(M + H)⁺ 10301-(4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}phenyl)-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 471 (M + H)⁺ 10311-{4-[1-(cinnolin-4-ylcarbonyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 506 (M + H)⁺ 10321-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinolin-7- ESI(+))ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 505 (M + H)⁺ 10331-{4-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 497 (M + H)⁺ 10341-(4-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 485 (M + H)⁺1035 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(5,6,7,8- ESI(+))tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 509 (M +H)⁺ 1036 1-{4-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6- ESI(+))ylcarbonyl)piperidin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 511ylmethyl)urea (M + H)⁺ 10371-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-7- ESI(+))ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 505 (M + H)⁺ 10381-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(quinoxalin-2- ESI(+))ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 506 (M + H)⁺ 10391-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(2- ESI(+))methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea m/e 511 (M +H)⁺ 10401-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2E)-3-(pyridin-2- ESI(+))yl)prop-2-enoyl]piperidin-4-yl}phenyl)urea m/e 481 (M + H)⁺ 10411-(4-{1-[(4-chloro-2,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-ESI(+)) yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e XXX (M +H)⁺ 1042 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(8- ESI(+))methylimidazo[1,2-a]pyridin-2-yl)carbonyl]piperidin-4- m/e 517yl}phenyl)urea (M + H)⁺ 10431-(4-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}phenyl)-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 499 (M + H)⁺ 40441-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-4,5,6,7- ESI(+))tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 512(M + H)⁺ 10451-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methyl-4H- ESI(+))furo[3,2-b]pyrrol-5-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 497 (M +H)⁺ 1046 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2,3-ESI(+)) dihydro-1-benzofuran-5-yl)carbonyl]piperidin-4-yl}phenyl)uream/e 510 (M + H)⁺ 10471-(4-{1-[(4-chloro-1-ethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 506 (M + H)⁺1048 1-{4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 497 (M + H)⁺ 10491-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(isoquinolin-8- ESI(+))ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 505 (M + H)⁺ 10501-(4-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}phenyl)-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 493 (M + H)⁺ 10511-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(3-methoxythiophen-ESI(+)) 2-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 490 (M + H)⁺ 10521-{4-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 497 (M + H)⁺ 10531-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(4,5,6,7-tetrahydro-ESI(+)) 1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 515(M + H)⁺ 10541-{4-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 511 (M + H)⁺ 10551-(4-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 473 (M + H)⁺ 10561-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[3-methyl-1-(prop-2-ESI(+)) en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)phenyl]urea m/e498 (M + H)⁺ 10571-{4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512 (M + H)⁺ 10581-(4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}phenyl)-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 489 (M + H)⁺ 10591-(4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 483 (M + H)⁺ 10601-{4-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 511 (M + H)⁺ 10651-(4-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}phenyl)-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 517 (M + H)⁺ 10661-(4-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 492 (M + H)⁺ 11211-(4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 501 (M + H)⁺1122 1-{4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]phenyl}-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 511 (M + H)⁺ 11231-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H- ESI(+))indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 508 (M + H)⁺ 11241-(4-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5- ESI(+))yl)carbonyl]piperidin-4-yl}phenyl)-3-(imidazo[1,2-a]pyridin-7- m/e 506ylmethyl)urea (M + H)⁺ 11251-(4-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 483 (M + H)⁺ 11261-(4-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 514 (M + H)⁺1127 1-(4-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 471 (M + H)⁺1128 1-(4-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-ESI(+)) yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 501 (M +H)⁺ 11291-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(thieno[3,2-b]furan-5-ESI(+)) ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 500 (M + H)⁺ 11301-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxythiophen-ESI(+)) 2-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 490 (M + H)⁺ 11311-(4-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 485 (M + H)⁺ 11321-(4-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 495 (M + H)⁺1133 1-{4-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]phenyl}-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 515 (M + H)⁺ 11341-[4-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4- ESI(+))yl]carbonyl}piperidin-4-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7- m/e 514ylmethyl)urea (M + H)⁺ 11351-{4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 494 (M + H)⁺ 11361-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(4-methoxy-5- ESI(+))methylpyridin-2-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 499 (M + H)⁺1137 1-(4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-ESI(+)) yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512 (M +H)⁺ 11381-(4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}phenyl)-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 495 (M + H)⁺ 11391-(4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}phenyl)-3-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 485 (M + H)⁺ 11401-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[4-(propan-2- ESI(+))yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)phenyl]urea m/e 498 (M + H)⁺1141 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-5-propyl-ESI(+)) 1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 500 (M +H)⁺ 11421-(4-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 512 (M + H)⁺1143 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(pyrazolo[1,5- ESI(+))a]pyridin-2-ylcarbonyl)piperidin-4-yl]phenyl}urea m/e 494 (M + H)⁺ 11441-{4-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]phenyl}-3- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 494 (M + H)⁺ 11451-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2-(propan-2-yl)-1,3-ESI(+)) oxazol-4-yl]carbonyl}piperidin-4-yl)phenyl]urea m/e 487 (M + H)⁺1146 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H- ESI(+))indazol-7-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 508 (M + H)⁺ 11471-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methoxy-5- ESI(+))methylpyridin-3-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 499 (M + H)⁺1148 1-(4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4- ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 515 (M + H)⁺1149 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H- ESI(+))indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 508 (M + H)⁺ 11501-(4-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}phenyl)-ESI(+)) 3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 517 (M + H)⁺ 11511-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(2-methyl-2H- ESI(+))indazol-6-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 508 (M + H)⁺ 11521-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{1-[(1-methyl-1H- ESI(+))indazol-4-yl)carbonyl]piperidin-4-yl}phenyl)urea m/e 508 (M + H)⁺ 11531-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-{[2- ESI(+))(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)phenyl]urea m/e 512(M + H)⁺

Example 230B4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 2-hydroxy-2-methylpropanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆/D₂O, Temp=90° C.) δ ppm8.77 (dd, J=6.9, 0.9 Hz, 1H), 8.22-8.18 (m, 1H), 8.02-7.98 (m, 1H),7.88-7.81 (m, 2H), 7.77 (s, 1H), 7.44 (dd, J=6.9, 1.6 Hz, 1H), 7.40-7.34(m, 2H), 4.76-4.64 (m, 4H), 2.98-2.82 (m, 3H), 1.89-1.81 (m, 2H),1.65-1.48 (m, 2H), 1.38 (s, 6H); MS (ESI(+)) m/e 421 (M+H)⁺.

TABLE 13 The following Examples were prepared essentially as describedin Example 230, substituting the appropriate carboxylic acid in Example230B. Ex Name MS 231N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-3- (ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 443 (M + H)⁺ 232N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-(ESI(+)) ylcarbonyl)piperidin-4-yl]benzamide m/e 447 (M + H)⁺ 2334-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 445 (M + H)⁺ 2344-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]piperidin-(ESI(+)) 4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 495(M + H)⁺ 235N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydrofuran-2- (ESI(+))ylacetyl)piperidin-4-yl]benzamide m/e 447 (M + H)⁺ 236N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-(ESI(+)) ylacetyl)piperidin-4-yl]benzamide m/e 461 (M + H)⁺ 237N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(propan-2- (ESI(+))yloxy)acetyl]piperidin-4-yl}benzamide m/e 435 (M + H)⁺ 238N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2- (ESI(+))methylbutanoyl]piperidin-4-yl}benzamide m/e 419 (M + H)⁺ 239N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- (ESI(+))methylpropanoyl)piperidin-4-yl]benzamide m/e 405 (M + H)⁺ 308N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3S)-tetrahydrofuran-3-(ESI(+)) ylcarbonyl]piperidin-4-yl}benzamide m/e 433 (M + H)⁺ 309N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3R)-tetrahydrofuran-3-(ESI(+)) ylcarbonyl]piperidin-4-yl}benzamide m/e 433 (M + H)⁺ 310N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2R)-tetrahydrofuran-2-(ESI(+)) ylcarbonyl]piperidin-4-yl}benzamide m/e 433 (M + H)⁺ 311N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-tetrahydrofuran-2-(ESI(+)) ylcarbonyl]piperidin-4-yl}benzamide m/e 433 (M + H)⁺ 3124-[1-(cyclopropylacetyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 417 (M + H)⁺ 3134-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 377 (M + H)⁺ 4374-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 439 (M + H)⁺ 444-{1-[(3,3-difluorocyclobutyl)carbonyl]piperidin-4-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 453 (M + H)⁺ 4414-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 481 (M + H)⁺ 4844-[1-(furan-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 429 (M + H)⁺ 498N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2- (ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 440 (M + H)⁺ 4994-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 433 (M + H)⁺ 500N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4- (ESI(+))methylbenzoyl)piperidin-4-yl]benzamide m/e 453 (M + H)⁺ 5014-[1-(2,2-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 433 (M + H)⁺ 5024-[1-(cyclohexylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 445 (M + H)⁺ 503N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2- (ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 445 (M + H)⁺ 504N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3,3,3- (ESI(+))trifluoropropanoyl)piperidin-4-yl]benzamide m/e 445 (M + H)⁺ 5054-(1-butanoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 405 (M + H)⁺ 5064-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 475 (M + H)⁺ 507N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- (ESI(+))methylbenzoyl)piperidin-4-yl]benzamide m/e 453 (M + H)⁺ 5084-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 457 (M + H)⁺ 5094-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 419 (M + H)⁺ 510N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylpent-2- (ESI(+))enoyl]piperidin-4-yl}benzamide m/e 431 (M + H)⁺ 511N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-(ESI(+)) 5-yl)carbonyl]piperidin-4-yl}benzamide m/e 443 (M + H)⁺ 512N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyloxetan-3- (ESI(+))yl)carbonyl]piperidin-4-yl}benzamide m/e 433 (M + H)⁺ 5134-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 457 (M + H)⁺ 5144-{1-[(1-cyanocyclopropyl)carbonyl]piperidin-4-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 428 (M + H)⁺ 5154-[1-(cyclopentylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 431 (M + H)⁺ 5164-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 457 (M + H)⁺ 517N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-(ESI(+)) 4-yl)carbonyl]piperidin-4-yl}benzamide m/e 443 (M + H)⁺ 518N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- (ESI(+))oxobutanoyl)piperidin-4-yl]benzamide m/e 419 (M + H)⁺ 5194-{1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 457 (M + H)⁺ 5204-[1-(4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 464 (M + H)⁺ 5214-[1-(3-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 464 (M + H)⁺ 5224-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 475 (M + H)⁺ 523N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2- (ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 441 (M + H)⁺ 524N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2- (ESI(+))yl)carbonyl]piperidin-4-yl}benzamide m/e 459 (M + H)⁺ 5254-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]piperidin-4-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 458 (M + H)⁺ 526N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- (ESI(+))methoxybenzoyl)piperidin-4-yl]benzamide m/e 469 (M + H)⁺ 5274-[1-(3-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 473 (M + H)⁺ 528N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4- (ESI(+))methoxybenzoyl)piperidin-4-yl]benzamide m/e 469 (M + H)⁺ 5294-[1-(4-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 473 (M + H)⁺ 5304-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 475 (M + H)⁺ 5314-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 403 (M + H)⁺ 532N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-propanoylpiperidin-4- (ESI(+))yl)benzamide m/e 391 (M + H)⁺ 533N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-(ESI(+)) yl)carbonyl]piperidin-4-yl}benzamide m/e 442 (M + H)⁺ 534N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- (ESI(+))methylbutanoyl)piperidin-4-yl]benzamide m/e 419 (M + H)⁺ 535N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4- (ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 440 (M + H)⁺ 5364-[1-(2,3-dimethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 433 (M + H)⁺ 537N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3- (ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 440 (M + H)⁺ 538N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1- (ESI(+))methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide m/e 417 (M + H)⁺ 539N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- (ESI(+))methoxybenzoyl)piperidin-4-yl]benzamide m/e 469 (M + H)⁺ 6994-[1-(2-chlorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 473 (M + H)⁺ 7004-[1-(2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 475 (M + H)⁺ 7014-[1-(3,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 475 (M + H)⁺ 702N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3- (ESI(+))(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide m/e 507 (M + H)⁺ 703N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3- (ESI(+))(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide m/e 523 (M + H)⁺ 704N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4- (ESI(+))(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide m/e 523 (M + H)⁺ 705N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[4- (ESI(+))(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide m/e 507 (M + H)⁺ 706N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2- (ESI(+))(trifluoromethoxy)benzoyl]piperidin-4-yl}benzamide m/e 523 (M + H)⁺ 707N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylacetyl)piperidin-(ESI(+)) 4-yl]benzamide m/e 453 (M + H)⁺ 708N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2- (ESI(+))(trifluoromethyl)benzoyl]piperidin-4-yl}benzamide m/e 507 (M + H)⁺ 7374-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 464 (M + H)⁺ 9134-{1-[(2-chloropyridin-3-yl)carbonyl]piperidin-4-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 474 (M + H)⁺ 914N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3-methylbut-2- ESI(+))enoyl)piperidin-4-yl]benzamide m/e 417 (M + H)⁺ 9154-[1-(3-fluoro-4-methoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 487 (M + H)⁺ 916N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methylcyclopent-1- ESI(+))en-1-yl)carbonyl]piperidin-4-yl}benzamide m/e 443 (M + H)⁺ 9174-[1-(2-ethylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ESI(+)) ylmethyl)benzamide m/e 433 (M + H)⁺ 9184-{1-[(4-fluorophenoxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 487 (M + H)⁺ 9194-[1-(3,5-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 499 (M + H)⁺ 9204-[1-(cyclohex-3-en-1-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 443 (M + H)⁺ 921N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2- ESI(+))methoxyphenyl)acetyl]piperidin-4-yl}benzamide m/e 483 (M + H)⁺ 9224-[1-(3-hydroxy-2-phenylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 483 (M + H)⁺ 923N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- ESI(+))methylbenzoyl)piperidin-4-yl]benzamide m/e 453 (M + H)⁺ 9244-[1-(2-acetylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ESI(+)) ylmethyl)benzamide m/e 481 (M + H)⁺ 925N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[2- ESI(+))(methoxymethyl)benzoyl]piperidin-4-yl}benzamide m/e 483 (M + H)⁺ 926N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- ESI(+))phenylpropanoyl)piperidin-4-yl]benzamide m/e 467 (M + H)⁺ 9274-[1-(2,6-dimethoxybenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 499 (M + H)⁺ 9284-[1-(N,N-diethyl-beta-alanyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 462 (M + H)⁺ 929N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[(2- ESI(+))methylpropyl)sulfonyl]acetyl}piperidin-4-yl)benzamide m/e 497 (M + H)⁺930 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- ESI(+))phenoxypropanoyl)piperidin-4-yl]benzamide m/e 483 (M + H)⁺ 931N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-({[(1R,2S)-2- ESI(+))methylcyclohexyl]oxy}acetyl)piperidin-4-yl]benzamide m/e 489 (M + H)⁺932 4-{1-[(2-chloro-6-methylpyridin-4-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 488 (M + H)⁺ 933N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3- ESI(+))methoxyphenyl)acetyl]piperidin-4-yl}benzamide m/e 483 (M + H)⁺ 9344-[1-(2-chloro-4-cyanobenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 498 (M + H)⁺ 935N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-2-methylbut-2- ESI(+))enoyl]piperidin-4-yl}benzamide m/e 417 (M + H)⁺ 936N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5- ESI(+))methylphenyl)acetyl]piperidin-4-yl}benzamide m/e 497 (M + H)⁺ 9374-[1-(2-hydroxy-3-methylbenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 469 (M + H)⁺ 959N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H- ESI(+))pyrazol-3-yl]carbonyl}piperidin-4-yl)benzamide m/e 471 (M + H)⁺ 9604-{1-[(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-ESI(+)) 4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 483 (M +H)⁺ 961 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-4,5,6,7-ESI(+)) tetrahydro-2H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide m/e497 (M + H)⁺ 962N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-2,1-ESI(+)) benzoxazol-3-ylcarbonyl)piperidin-4-yl]benzamide m/e 484 (M +H)⁺ 963 4-{1-[(3-fluoro-6-methylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 472 (M + H)⁺ 9644-{1-[(2-chloro-3-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 492 (M + H)⁺ 9654-{1-[(3-chloropyridin-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 474 (M + H)⁺ 966N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(pyridin-2- ESI(+))yl)cyclopropyl]carbonyl}piperidin-4-yl)benzamide m/e 480 (M + H)⁺ 9674-{1-[(1-cyclopentyl-1H-pyrazol-3-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 497 (M + H)⁺ 9684-{1-[2-(3-fluorophenoxy)propanoyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 501 (M + H)⁺ 9694-(1-{[1-(difluoromethyl)-1H-pyrazol-5-yl]carbonyl}piperidin-4- ESI(+))yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 479 (M + H)⁺ 9704-[1-(3,4-dihydro-2H-chromen-6-ylcarbonyl)piperidin-4-yl]-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 495 (M + H)⁺ 9714-{1-[(cyclohexyloxy)acetyl]piperidin-4-yl}-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 475 (M + H)⁺ 9724-{1-[(2-chloropyridin-3-yl)acetyl]piperidin-4-yl}-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 488 (M + H)⁺ 9734-{1-[(5-cyclopropyl-1,2-oxazol-3-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 470 (M + H)⁺ 9744-[1-(2H-chromen-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 493 (M + H)⁺ 9754-{1-[(3,5-difluoropyridin-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 476 (M + H)⁺ 9764-[1-(2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl)piperidin-4-yl]-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 497 (M + H)⁺ 977N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4- ESI(+))methoxycyclohexyl)carbonyl]piperidin-4-yl}benzamide m/e 475 (M + H)⁺ 9784-[1-(2,3-dihydro-1,4-benzodioxin-5-ylcarbonyl)piperidin-4-yl]-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 497 (M + H)⁺ 979N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-4- ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 490 (M + H)⁺ 980N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-1,3- ESI(+))benzoxazol-6-yl)carbonyl]piperidin-4-yl}benzamide m/e 494 (M + H)⁺ 9814-{1-[(1-tert-butyl-3-methyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-ESI(+)) yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 499 (M +H)⁺ 982 4-{1-[(1-cyanocyclopentyl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 456 (M + H)⁺ 983N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thieno[3,2-b]pyridin-2-ESI(+)) ylcarbonyl)piperidin-4-yl]benzamide m/e 496 (M + H)⁺ 984N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinolin-7- ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 490 (M + H)⁺ 9854-[1-(5-cyano-2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 482 (M + H)⁺ 986N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(5,6,7,8- ESI(+))tetrahydroquinolin-3-ylcarbonyl)piperidin-4-yl]benzamide m/e 494 (M +H)⁺ 9874-[1-(3,4-dihydro-2H-pyrano[2,3-b]pyridin-6-ylcarbonyl)piperidin-ESI(+)) 4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 496 (M +H)⁺ 988 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-7-ESI(+)) ylcarbonyl)piperidin-4-yl]benzamide m/e 490 (M + H)⁺ 989N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(quinoxalin-2- ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 491 (M + H)⁺ 990N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(2- ESI(+))methoxypyridin-3-yl)prop-2-enoyl]piperidin-4-yl}benzamide m/e 496 (M +H)⁺ 991 -(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2E)-3-(pyridin-2-ESI(+)) yl)prop-2-enoyl]piperidin-4-yl}benzamide m/e 466 (M + H)⁺ 992N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(8-methylimidazo[1,2- ESI(+))a]pyridin-2-yl)carbonyl]piperidin-4-yl}benzamide m/e 493 (M + H)⁺ 9934-{1-[(2-ethoxypyridin-4-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 484 (M + H)⁺ 994N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-4,5,6,7- ESI(+))tetrahydro-1H-indazol-3-yl)carbonyl]piperidin-4-yl}benzamide m/e 497(M + H)⁺ 995N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methyl-4H-furo[3,2-ESI(+)) b]pyrrol-5-yl)carbonyl]piperidin-4-yl}benzamide m/e 482 (M + H)⁺996 4-[1-(3-cyano-5-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 482 (M + H)⁺ 997N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(isoquinolin-8- ESI(+))ylcarbonyl)piperidin-4-yl]benzamide m/e 490 (M + H)⁺ 9984-{1-[(4-cyanophenyl)acetyl]piperidin-4-yl}-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 478 (M + H)⁺ 9994-[1-(3-cyano-4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 482 (M + H)⁺ 1000N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4,5,6,7-tetrahydro-1,3-ESI(+)) benzothiazol-2-ylcarbonyl)piperidin-4-yl]benzamide m/e 500 (M +H)⁺ 10014-[1-(1,3-benzothiazol-2-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 496 (M + H)⁺ 10024-{1-[(3-ethyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 458 (M + H)⁺ 1003N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[3-methyl-1-(prop-2- ESI(+))en-1-yl)-1H-pyrazol-5-yl]carbonyl}piperidin-4-yl)benzamide m/e 483 (M +H)⁺ 1004 4-[1-(1,2,3-benzothiadiazol-5-ylcarbonyl)piperidin-4-yl]-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 497 (M + H)⁺1005 4-{1-[(2-ethyl-1,3-thiazol-4-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 474 (M + H)⁺ 1006N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2- ESI(+))yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)benzamide m/e 483 (M + H)⁺1007 4-{1-[(5,6-dimethylpyridin-3-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 468 (M + H)⁺ 1008N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2- ESI(+))yl)tetrahydro-2H-pyran-4-yl]carbonyl}piperidin-4-yl)benzamide m/e 489(M + H)⁺ 1009 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methoxy-6-ESI(+)) methylbenzoyl)piperidin-4-yl]benzamide m/e 483 (M + H)⁺ 10104-[1-(1,3-benzothiazol-7-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 496 (M + H)⁺ 10614-{1-[(2-chloro-5-fluoropyridin-4-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 493 (M + H)⁺ 10624-{1-[(3-cyclopropyl-1,2-oxazol-5-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 471 (M + H)⁺ 1063N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{l-[(3-methoxythiophen-2- ESI(+))yl)carbonyl]piperidin-4-yl}benzamide m/e 476 (M + H)⁺ 1064N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-methyl-5-(propan-2-ESI(+)) yl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide m/e 486 (M + H)⁺1084 4-{1-[(2-cyclopropyl-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 486 (M + H)⁺1085 4-[1-(1,3-benzothiazol-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 496 (M + H)⁺ 1086N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol- ESI(+))6-yl)carbonyl]piperidin-4-yl}benzamide m/e 493 (M + H)⁺ 10874-{1-[(4-chloro-1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-ESI(+)) yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 491 (M +H)⁺ 10884-{1-[(5-ethylpyridin-2-yl)carbonyl]piperidin-4-yl}-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 468 (M + H)⁺ 10894-{1-[(3-chloro-5-cyanopyridin-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 499 (M + H)⁺ 10904-{1-[(1-cyano-3-methylcyclobutyl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 456 (M + H)⁺ 10914-{1-[(1,5-diethyl-1H-1,2,3-triazol-4-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 486 (M + H)⁺1092 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxythiophen-2-ESI(+)) yl)carbonyl]piperidin-4-yl}benzamide m/e 475 (M + H)⁺ 10934-{1-[(5-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 470 (M + H)⁺ 10944-{1-[(5-cyclopropylpyridin-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 480 (M + H)⁺ 10954-[1-(4-cyano-2,6-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 500 (M + H)⁺ 10964-(1-{[1-ethyl-3-(propan-2-yl)-1H-pyrazol-4-yl]carbonyl}piperidin-ESI(+)) 4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 499 (M +H)⁺ 1097 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[1-(propan-2-yl)-1H-ESI(+)) pyrazol-3-yl]acetyl}piperidin-4-yl)benzamide m/e 485 (M + H)⁺1098 4-[1-(1-benzofuran-3-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2-ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 479 (M + H)⁺ 1099 Example1099 ESI(+))N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methyl-5,6,7,8- m/e 497tetrahydroimidazo[1,5-a]pyridin-1-yl)carbonyl]piperidin-4- (M + H)⁺yl}benzamide 1100N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(4-methoxy-5- ESI(+))methylpyridin-2-yl)carbonyl]piperidin-4-yl}benzamide m/e 484 (M + H)⁺1101 4-{1-[(1-cyclopentyl-1H-pyrazol-5-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 497 (M + H)⁺1102 4-{1-[(4-chloro-1,3-thiazol-5-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 480 (M + H)⁺1103 4-{1-[(3-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 470 (M + H)⁺ 1104N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[4-(propan-2- ESI(+))yl)pyrimidin-5-yl]carbonyl}piperidin-4-yl)benzamide m/e 483 (M + H)⁺1105 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-5-propyl-ESI(+)) 1H-pyrazol-4-yl)carbonyl]piperidin-4-yl}benzamide m/e 485 (M +H)⁺ 11064-{1-[2-(3-cyclopropyl-1H-pyrazol-1-yl)propanoyl]piperidin-4-yl}-ESI(+)) N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 497 (M + H)⁺1107 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2,3-dihydro-ESI(+)) 1-benzofuran-7-yl)carbonyl]piperidin-4-yl}benzamide m/e 495 (M +H)⁺ 1108N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3- ESI(+))thiazol-4-yl]carbonyl}piperidin-4-yl)benzamide m/e 488 (M + H)⁺ 11094-(1-{[1-(difluoromethyl)-5-methyl-1H-pyrazol-3- ESI(+))yl]carbonyl}piperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7- m/e 493ylmethyl)benzamide (M + H)⁺ 11104-{1-[(4-cyanothiophen-2-yl)carbonyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 470 (M + H)⁺ 1111N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazolo[1,5-a]pyridin-ESI(+)) 2-ylcarbonyl)piperidin-4-yl]benzamide m/e 479 (M + H)⁺ 11124-[1-(1-benzofuran-5-ylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2- ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 479 (M + H)⁺ 1113N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2-(propan-2-yl)-1,3- ESI(+))oxazol-4-yl]carbonyl}piperidin-4-yl)benzamide m/e 472 (M + H)⁺ 1114N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methoxy-5- ESI(+))methylpyridin-3-yl)carbonyl]piperidin-4-yl}benzamide m/e 484 (M + H)⁺1115 4-{1-[(5,6-dimethoxypyridin-2-yl)carbonyl]piperidin-4-yl}-N-ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 500 (M + H)⁺1116 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol-ESI(+)) 4-yl)carbonyl]piperidin-4-yl}benzamide m/e 493 (M + H)⁺ 11174-{1-[(2-ethylpiperidin-1-yl)(oxo)acetyl]piperidin-4-yl}-N- ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 502 (M + H)⁺ 1118N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2-methyl-2H-indazol- ESI(+))6-yl)carbonyl]piperidin-4-yl}benzamide m/e 493 (M + H)⁺ 1119N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-indazol- ESI(+))4-yl)carbonyl]piperidin-4-yl}benzamide m/e 493 (M + H)⁺ 1120N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-{[2- ESI(+))(trifluoromethyl)furan-3-yl]carbonyl}piperidin-4-yl)benzamide m/e 497(M + H)⁺

Example 2404-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 215,substituting 3-methoxypropanoyl chloride for 2-cyclopentylacetylchloride in Example 215B. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.08 (t, J=5.8Hz, 1H), 8.46 (dd, J=1.9, 0.9 Hz, 1H), 7.94 (dd, J=1.2, 0.6 Hz, 1H),7.91-7.85 (m, 2H), 7.79-7.73 (m, 2H), 7.56-7.49 (m, 2H), 7.43-7.39 (m,2H), 7.38-7.33 (m, 2H), 7.20 (dd, J=9.2, 1.7 Hz, 1H), 5.00 (bs, 2H),4.45 (d, J=5.8 Hz, 2H), 3.54 (t, J=6.2 Hz, 2H), 3.17 (s, 3H), 2.43-2.35(m, 2H); MS (ESI(+)) m/e 468 (M+H)⁺.

Example 2415-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 241A5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

A solution of 5-bromothiophene-2-carboxylic acid (1.279 g, 6.18 mmol),imidazo[1,2-a]pyridin-7-ylmethanamine (1 g, 6.79 mmol),1-hydroxybenzotriazole hydrate (1.041 g, 6.79 mmol) andN-methylmorpholine (1.698 ml, 15.44 mmol) in dimethylformamide (20 ml)at room temperature was treated with1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (2.131 g,11.12 mmol). The mixture was stirred overnight and poured into a gentlystirred round-bottom flask containing water (100 ml) and ethyl acetate(30 ml). The resulting bilayer suspension was stirred for severalminutes, filtered and washed with water then minimal ethyl acetate togive the title compound after drying.

Example 241B tert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline.

Example 241CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 241D5-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting acetyl chloride for 2-cyclopentylacetyl chloride andN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.13-9.06(m, 1H), 8.48 (d, J=7.0 Hz, 1H), 7.88 (s, 1H), 7.72 (d, J=3.9 Hz, 1H),7.51 (d, J=1.2 Hz, 1H), 7.38 (s, 1H), 7.15 (t, J=4.2 Hz, 1H), 6.83 (dd,J=7.0, 1.6 Hz, 1H), 6.28-6.21 (m, 1H), 4.46 (d, J=5.9 Hz, 2H), 4.15-4.04(m, 2H), 3.61 (dt, J=11.3, 5.6 Hz, 2H), 2.63-2.35 (m, 2H), 2.07-1.99 (m,3H); MS (ESI)(+)) m/e 381 (M+H)⁺.

Example 242N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting methanesulfonyl chloride for 2-cyclopentylacetyl chlorideandN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.15-9.07(m, 1H), 8.48 (d, J=7.0 Hz, 1H), 7.88 (s, 1H), 7.73 (d, J=3.9 Hz, 1H),7.51 (s, 1H), 7.38 (bs, 1H), 7.17 (d, J=3.9 Hz, 1H), 6.83 (d, J=7.0 Hz,1H), 6.28 (bs, 1H), 4.49-4.43 (m, 2H), 3.88-3.82 (m, 2H), 3.29-3.07 (m,2H), 2.93 (s, 3H), 2.65-2.41 (m, 2H); MS (ESI)(+)) m/e 417 (M+H)⁺.

Example 2465-[1-(cyclopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting cyclopropyl sulfonyl chloride for 2-cyclopentylacetylchloride andN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.10 (t,J=6.0 Hz, 1H), 8.48 (d, J=7.0 Hz, 1H), 7.88 (s, 1H), 7.73 (d, J=3.9 Hz,1H), 7.51 (d, J=1.2 Hz, 1H), 7.38 (s, 1H), 7.17 (d, J=3.9 Hz, 1H), 6.83(dd, J=7.0, 1.6 Hz, 1H), 6.28 (bs, 1H), 4.46 (d, J=5.9 Hz, 2H),3.95-3.89 (m, 2H), 3.43 (t, J=5.7 Hz, 2H), 2.73-2.56 (m, 3H), 1.26-0.89(m, 4H); MS (ESI)(+)) m/e 443 (M+H)⁺.

Example 250N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[(4R)-2-oxo-4-(propan-2-yl)-1,3-oxazolidin-3-yl]thiophene-2-carboxamide

A solution of5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide (84mg, 0.25 mmol), (R)-4-isopropyloxazolidin-2-one (32 mg, 0.25 mmol),N,N-dimethylethane-1,2-diamine (2 mg, 0.025 mmol), copper(I) iodide (5mg, 0.025 mmol) and potassium carbonate (121 mg, 0.88 mmol) in dioxane(1 ml) was stirred at 110° C. overnight. Concentration and reverse phasechromatography provided the title compound. ¹H NMR (400 MHz,methanol-d₄) δ ppm 9.13 (t, J=5.3 Hz, 1H), 8.74 (d, J=5.5 Hz, 1H), 8.17(s, 1H), 7.99 (s, 1H), 7.79 (s, 1H), 7.62 (d, J=4.1 Hz, 1H), 7.47 (d,J=7.0 Hz, 1H), 6.77 (d, J=4.2 Hz, 1H), 4.72 (s, 2H), 4.61-4.42 (m, 3H),2.46 (ddd, J=10.2, 6.9, 3.5 Hz, 1H), 1.00 (d, J=7.0 Hz, 3H), 0.85 (d,J=6.8 Hz, 3H); (APCI(+)) m/e 385 (M+H)⁺.

Example 257N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methoxyacetyl)piperidin-4-yl]thiophene-2-carboxamideExample 257A tert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1B, substitutingtert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor N-isopentyl-4-nitrobenzamide.

Example 257BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 257CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methoxyacetyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and methoxyacetic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.39 (d, J=7.0 Hz, 1H), 7.79(s, 1H), 7.60 (d, J=3.8 Hz, 1H), 7.53 (d, J=1.3 Hz, 1H), 7.44 (s, 1H),6.96 (d, J=3.8 Hz, 1H), 6.92 (dd, J=7.1, 1.2 Hz, 1H), 4.58 (bs, 2H),3.85-3.76 (m, 2H), 3.03 (tt, J=11.8, 3.8 Hz, 1H), 2.97-2.82 (m, 5H),2.18-2.09 (m, 2H), 1.96 (s, 1H), 1.86-1.71 (m, 2H); MS (ESI(+)) m/e 413(M+H)⁺.

TABLE 14 The following Examples were prepared essentially as describedin Example 257, substituting the appropriate carboxylic acid in Example257C. Ex Name MS 2585-(1-acetylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)thiophene-2-carboxamide m/e 383 (M + H)⁺ 259N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2- (ESI(+))methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide m/e 411 (M + H)⁺260 5-[1-(cyclopropylcarbonyl)piperidin-4-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 409 (M + H)⁺ 261N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydrofuran-3- (ESI(+))ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide m/e 439 (M + H)⁺ 262N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-(ESI(+)) ylacetyl)piperidin-4-yl]thiophene-2-carboxamide m/e 467 (M +H)⁺ 263 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3- (ESI(+))methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide m/e 425 (M + H)⁺264 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(1,2-oxazol-5- (ESI(+))ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide m/e 436 (M + H)⁺ 879N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-methyl-2-(piperazin-(ESI(+)) 1-yl)propanoyl]piperidin-4-yl}thiophene-2-carboxamide m/e 495(M + H)⁺ 8875-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)thiophene-2-carboxamide m/e 481 (M + H)⁺ 8885-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)thiophene-2-carboxamide m/e 481 (M + H)⁺

Example 2665-[5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 250,substituting 5-(hydroxymethyl)oxazolidin-2-one for(R)-4-isopropyloxazolidin-2-one. ¹H NMR (400 MHz, methanol-d₄) δ ppm9.10 (s, 1H), 8.74 (d, J=7.0 Hz, 1H), 8.17 (d, J=2.0 Hz, 1H), 7.98 (d,J=2.1 Hz, 1H), 7.78 (s, 1H), 7.60 (d, J=4.2 Hz, 1H), 7.52-7.41 (m, 1H),6.60 (d, J=4.2 Hz, 1H), 4.84 (s, 1H), 4.71 (d, J=4.2 Hz, 2H), 4.16 (t,J=9.1 Hz, 1H), 3.98 (dd, J=8.9, 6.2 Hz, 1H), 3.88 (dd, J=12.7, 3.0 Hz,1H), 3.69 (dd, J=12.7, 3.6 Hz, 1H); (APCI(+)) m/e 373 (M+H)⁺.

Example 2675-[(4R)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 250,substituting (R)-5-hydroxyoxazolidin-2-one for(R)-4-isopropyloxazolidin-2-one. ¹H NMR (400 MHz, methanol-d₄) δ ppm9.10 (t, J=6.1 Hz, 1H), 8.73 (d, J=6.9 Hz, 1H), 8.16 (d, J=1.8 Hz, 1H),7.98 (d, J=2.0 Hz, 1H), 7.78 (s, 1H), 7.61 (d, J=4.2 Hz, 1H), 7.46 (d,J=7.7 Hz, 1H), 6.68 (d, J=4.2 Hz, 1H), 4.71 (s, 2H), 4.62 (t, J=5.7 Hz,1H), 4.15 (dd, J=10.9, 5.3 Hz, 1H), 3.83 (d, J=10.9 Hz, 1H), 2.97 (dd,J=17.7, 6.2 Hz, 1H), 2.50 (d, J=18.2 Hz, 1H); (APCI(+)) m/e 357 (M+H)⁺.

Example 2685-[(4S)-4-hydroxy-2-oxopyrrolidin-1-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 250,substituting (S)-5-hydroxyoxazolidin-2-one for(R)-4-isopropyloxazolidin-2-one. ¹H NMR (400 MHz, methanol-d₄) δ ppm9.10 (t, J=5.7 Hz, 1H), 8.74 (d, J=7.0 Hz, 1H), 8.17 (d, J=2.0 Hz, 1H),7.98 (d, J=2.1 Hz, 1H), 7.78 (s, 1H), 7.61 (d, J=4.2 Hz, 1H), 7.46 (d,J=7.0 Hz, 1H), 6.68 (d, J=4.2 Hz, 1H), 4.71 (s, 2H), 4.62 (t, J=5.7 Hz,1H), 4.15 (dd, J=10.9, 5.3 Hz, 1H), 3.83 (d, J=11.0 Hz, 1H), 2.97 (dd,J=17.6, 6.2 Hz, 1H), 2.50 (d, J=16.8 Hz, 1H); (APCI(+)) m/e 357 (M+H)⁺.

Example 271N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(methylsulfonyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting methanesulfonyl chloride for 2-cyclopentylacetyl chlorideandN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.39 (d,J=7.0 Hz, 1H), 7.79 (s, 1H), 7.60 (d, J=3.8 Hz, 1H), 7.53 (d, J=1.3 Hz,1H), 7.44 (s, 1H), 6.96 (d, J=3.8 Hz, 1H), 6.92 (dd, J=7.1, 1.2 Hz, 1H),4.58 (bs, 2H), 3.85-3.76 (m, 2H), 3.03 (tt, J=11.8, 3.8 Hz, 1H),2.97-2.82 (m, 5H), 2.18-2.09 (m, 2H), 1.96 (s, 1H), 1.86-1.71 (m, 2H);MS (ESI(+)) m/e 419 (M+H)⁺.

Example 274N-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamideExample 274A tert-butyl4-(3-(imidazo[1,2-a]pyridin-6-ylmethyl)ureido)phenylcarbamate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-aminophenylcarbamate for 4-amino-N-isopentylbenzamide andimidazo[1,2-a]pyridin-6-ylmethanamine for imidazo[1,2-a]pyridin-6-amine.

Example 274B 1-(4-aminophenyl)-3-(imidazo[1,2-a]pyridin-6-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(3-(imidazo[1,2-a]pyridin-6-ylmethyl)ureido)phenylcarbamate fortert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 274CN-(4-{[(imidazo[1,2-a]pyridin-6-ylmethyl)carbamoyl]amino}phenyl)-4-methylpentanamide

The title compound was prepared as described in Example 1A, substituting1-(4-aminophenyl)-3-(imidazo[1,2-a]pyridin-6-ylmethyl)urea for3-methylbutan-1-amine and 4-methylpentanoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.70 (s, 1H), 8.50 (s, 1H), 8.43(s, 1H), 7.94 (s, 1H), 7.53 (m, 2H), 7.43 (m, 2H), 7.30 (m, 2H), 7.21(dd, J=9.2, 1.7 Hz, 1H), 6.61 (t, J=5.9 Hz, 1H), 4.28 (d, J=5.8 Hz, 2H),2.26 (t, J=7.6 Hz, 2H), 1.60-1.40 (m, 3H), 0.89 (d, J=6.4 Hz, 6H); MS(ESI(+)) m/e 380 (M+H)⁺.

TABLE 15 The following Examples were prepared essentially as describedin Example 274, substituting the appropriate carboxylic acid in Example274C. Ex Name ¹H NMR MS 275 3-cyclopentyl-N- ¹H NMR (400 MHz, DMSO-d₆) δppm 9.69 (s, (ESI(+)) (4-{[(imidazo[1,2- 1H), 8.48 (s, 1H), 8.43 (s,1H), 7.94 (s, 1H), m/e 406 a]pyridin-6- 7.53 (m, 2H), 7.43 (m, 2H), 7.30(m, 2H), 7.20 (M + H)⁺ ylmethyl)carba- (dd, J = 9.2, 1.7 Hz, 1H), 6.60(t, J = 5.9 Hz, moyl]amino}phenyl) 1H), 4.28 (d, J = 5.8 Hz, 2H), 2.26(t, J = 7.6 propanamide Hz, 2H), 1.75 (m, 3H), 1.66-1.39 (m, 6H), 1.08(m, 2H) 276 N-(4- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.36 (s, (ESI(+)){[(imidazo[1,2- 1H), 8.53 (s, 1H), 8.43 (s, 1H), 7.94 (s, 1H), m/e 382a]pyridin-6- 7.53 (m, 2H), 7.49 (m, 2H), 7.33 (m, 2H), 7.21 (M + H)⁺ylmethyl)carba- (dd, J = 9.2, 1.7 Hz, 1H), 6.62 (t, J = 5.9 Hz,moyl]amino}phenyl)- 1H), 4.28 (d, J = 5.9 Hz, 2H), 3.97 (s, 2H), 3.672-(propan-2- (m, 1H), 1.16 (d, J = 6.1 Hz, 6H) yloxy)acetamide 277 N-(4-¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.74 (s, (ESI(+)) {[(imidazo[1,2- 1H),8.50 (s, 1H), 8.44 (d, J = 1.5 Hz, 1H), 7.96 m/e 394 a]pyridin-6- (s,1H), 7.54 (m, 2H), 7.44 (m, 2H), 7.31 (m, (M + H)⁺ ylmethyl)carba- 2H),7.22 (dd, J = 9.2, 1.7 Hz, 1H), 6.61 (t, J = moyl]amino}phenyl)- 5.9 Hz,1H), 4.28 (d, J = 5.9 Hz, 2H), 4.12 (m, 2-(tetrahydrofuran- 1H), 3.74(m, 1H), 3.60 (m, 1H), 2.47 (m, 1H), 2-yl)acetamide 2.39 (m, 1H), 1.98(m, 1H), 1.81 (m, 2H), 1.49 (m, 1H) 278 N-(4- ¹H NMR (500 MHz, DMSO-d₆)δ ppm 9.72 (s, (ESI(+)) {[(imidazo[1,2- 1H), 8.50 (s, 1H), 8.43 (s, 1H),7.94 (s, 1H), m/e 408 a]pyridin-6- 7.53 (m, 2H), 7.43 (m, 2H), 7.31 (m,2H), 7.21 (M + H)⁺ ylmethyl)carba- (dd, J = 9.2, 1.7 Hz, 1H), 6.60 (t, J= 5.9 Hz, moyl]amino}phenyl)- 1H), 4.28 (d, J = 5.9 Hz, 2H), 3.82 (m,2H), 2-(tetrahydro- 3.29 (m, 2H), 2.20 (d, J = 7.1 Hz, 2H), 2.01 (m,2H-pyran-4- 1H), 1.57 (m, 2H), 1.25 (m, 2H) yl)acetamide 279 N-(4- ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.73 (s, (ESI(+)) {[(imidazo[1,2- 1H), 8.49(s, 1H), 8.42 (s, 1H), 7.94 (s, 1H), m/e 414 a]pyridin-6- 7.53 (m, 2H),7.42 (m, 2H), 7.35-7.15 (m, 8H), (M + H)⁺ ylmethyl)carba- 6.60 (t, J =5.9 Hz, 1H), 4.28 (d, J = 5.8 Hz, moyl]amino}phenyl)- 2H), 2.89 (t, J =7.3 Hz, 2H), 2.57 (t, J = 5.7 Hz, 3-phenylpropanamide 2H) 280 N-(4- ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.69 (s, (ESI(+)) {[(imidazo[1,2- 1H), 8.52(s, 1H), 8.47 (d, J = 7.0 Hz, 1H), 7.87 m/e 380 a]pyridin-7- (s, 1H),7.50 (bs, 1H), 7.42 (m, 2H), 7.37 (s, (M + H)⁺ ylmethyl)carba- 1H), 7.30(m, 2H), 6.82 (dd, J = 7.0, 1.5 Hz, moyl]amino}phenyl)- 1H), 6.63 (t, J= 6.0 Hz, 1H), 4.31 (d, J = 5.9 4-methylpentanamide Hz, 2H), 2.25 (t, J= 7.6 Hz, 2H), 1.60-1.41 (m, 3H), 0.88 (d, J = 6.4 Hz, 6H) 2813-cyclopentyl-N- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.69 (s, (ESI(+))(4-{[(imidazo[1,2- 1H), 8.53 (s, 1H), 8.48 (d, J = 6.9 Hz, 1H), 7.88 m/e406 a]pyridin-7- (bs, 1H), 7.52 (bs, 1H), 7.44 (m, 2H), 7.37 (s, (M +H)⁺ ylmethyl)carba- 1H), 7.31 (m, 2H), 6.83 (dd, J = 6.9, 1.4 Hz,moyl]amino}phenyl) 1H), 6.64 (t, J = 6.0 Hz, 1H), 4.32 (d, J = 5.9propanamide Hz, 2H), 2.27 (t, J = 7.6 Hz, 2H), 1.74 (m, 3H), 1.65-1.40(m, 6H), 1.09 (m, 2H) 282 N-(4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.37 (s,(ESI(+)) {[(imidazo[1,2- 1H), 8.59 (s, 1H), 8.49 (m, 1H), 7.89 (s, 1H),m/e 382 a]pyridin-7- 7.50 (m, 3H), 7.39 (s, 1H), 7.34 (m, 2H), 6.84 (M +H)⁺ ylmethyl)carba- (dd, J = 6.9, 1.6 Hz, 1H), 6.68 (t, J = 6.0 Hz,moyl]amino}phenyl)- 1H), 4.33 (d, J = 6.0 Hz, 2H), 3.98 (s, 2H), 3.672-(propan-2- (m, 1H), 1.16 (d, J = 6.1 Hz, 6H) yloxy)acetamide 283 N-(4-¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.73 (s, (ESI(+)) {[(imidazo[1,2- 1H),8.54 (s, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 m/e 394 a]pyridin-7- (s,1H), 7.51 (s, 1H), 7.44 (m, 2H), 7.38 (bs, (M + H)⁺ ylmethyl)carba- 1H),7.32 (m, 2H), 6.83 (dd, J = 6.9, 1.6 Hz, moyl]amino}phenyl)- 1H), 6.65(t, J = 6.0 Hz, 1H), 4.32 (d, J = 5.9 2-(tetrahydrofuran- Hz, 2H), 4.16(m, 1H), 3.76 (m, 1H), 3.60 (m, 2-yl)acetamide 1H), 2.50 (m, 1H), 2.39(m, 1H), 1.99 (m, 1H), 1.83 (m, 2H), 1.53 (m, 1H) 284 N-(4- ¹H NMR (400MHz, DMSO-d₆) δ ppm 9.72 (s, (ESI(+)) {[(imidazo[1,2- 1H), 8.53 (s, 1H),8.48 (d, J = 6.9 Hz, 1H), 7.88 m/e 408 a]pyridin-7- (bs, 1H), 7.51 (bs,1H), 7.44 (m, 2H), 7.38 (bs, (M + H)⁺ ylmethyl)carba- 1H), 7.32 (m, 2H),6.83 (m, 1H), 6.65 (m, 1H), moyl]amino}phenyl)- 4.32 (m, 2H), 3.82 (m,2H), 3.33 (m, 2H), 2.20 2-(tetrahydro- (d, J = 7.1 Hz, 2H), 1.97 (m,1H), 1.58 (m, 2H), 2H-pyran-4- 1.23 (m, 2H) yl)acetamide 285 N-(4- ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.74 (s, (ESI(+)) {[(imidazo[1,2- 1H), 8.54(s, 1H), 8.49 (d, J = 6.9 Hz, 1H), 7.89 m/e 414 a]pyridin-7- (bs, 1H),7.52 (bs, 1H), 7.42 (m, 3H), 7.35- (M + H)⁺ ylmethyl)carba- 7.22 (m,6H), 7.17 (m, 1H), 6.84 (d, J = 7.6 Hz, moyl]amino}phenyl)- 1H), 6.65(t, J = 6.0 Hz, 1H), 4.32 (d, J = 5.9 3-phenylpropanamide Hz, 2H), 2.90(t, J = 7.7 Hz, 2H), 2.58 (t, J = 7.7 Hz, 2H)

Example 290 tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylate Example 290A1-(4-bromo-2-fluorophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1C, substituting4-bromo-2-fluoroaniline for 4-amino-N-isopentylbenzamide andimidazo[1,2-a]pyridin-7-ylmethanamine for imidazo[1,2-a]pyridin-6-amine.

Example 290B tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromo-2-fluorophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.53-8.46 (m, 2H),8.09 (t, J=8.7 Hz, 1H), 7.91-7.88 (m, 1H), 7.54-7.50 (m, 1H), 7.42-7.37(m, 1H), 7.33-7.24 (m, 1H), 7.21-7.08 (m, 2H), 6.83 (dd, J=7.0, 1.7 Hz,1H), 6.17-6.10 (m, 1H), 4.35 (d, J=5.8 Hz, 2H), 4.01-3.94 (m, 2H),3.55-3.47 (m, 2H), 2.46-2.36 (m, 2H), 1.42 (s, 9H); MS (ESI(+)) m/e 466(M+H)⁺.

Example 291 tert-butyl(3S)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylateExample 291A (S)-tert-butyl 3-(4-nitrophenoxy)pyrrolidine-1-carboxylate

(S)-Tert-butyl 3-hydroxypyrrolidine-1-carboxylate (10 g, 53.4 mmol) wasdissolved in 1-fluoro-4-nitrobenzene (13.94 g, 99 mmol). An aqueoussolution of 5.9N potassium hydroxide (77 ml, 452 mmol) was addedfollowed by addition of tetrabutylammonium bromide (2.238 g, 6.94 mmol).The reaction mixture was stirred at 40° C. for 24 hours and then cooled,diluted with water and extracted with ethyl acetate. The combinedorganic layers were dried with sodium sulfate, filtered and concentratedto give the title compound.

Example 291B (S)-tert-butyl 3-(4-aminophenoxy)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1B, substituting(S)-tert-butyl 3-(4-nitrophenoxy)pyrrolidine-1-carboxylate forN-isopentyl-4-nitrobenzamide.

Example 291C tert-butyl(3S)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1C, substituting(S)-tert-butyl 3-(4-aminophenoxy)pyrrolidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm8.51-8.44 (m, 2H), 7.88-7.86 (m, 1H), 7.53-7.49 (m, 1H), 7.40-7.27 (m,3H), 6.86-6.80 (m, 3H), 6.63 (t, J=6.0 Hz, 1H), 4.93-4.84 (m, 1H), 4.32(d, J=6.0 Hz, 2H), 3.55-3.28 (m, 4H), 2.16-1.94 (m, 2H), 1.42-1.36 (m,9H); MS (ESI(+)) m/e 452 (M+H)⁺.

Example 292 tert-butyl{2-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}carbamate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(tert-butoxycarbonylamino)-3-fluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.26 (s, 1H), 9.08 (t, J=5.9 Hz,1H), 8.48 (dd, J=6.9, 0.9 Hz, 1H), 7.91-7.78 (m, 2H), 7.76-7.68 (m, 2H),7.52 (d, J=1.2 Hz, 1H), 7.39 (bs, 1H), 6.85 (dd, J=7.0, 1.7 Hz, 1H),4.49 (d, J=5.8 Hz, 2H), 1.48 (s, 9H); MS (ESI(+)) m/e 385 (M+H)⁺.

Example 2972-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamideExample 297A tert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiazol-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamidefor 4-bromoaniline.

Example 297BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1,2,3,6-tetrahydropyridin-4-yl)thiazole-5-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiazol-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 297C2-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1,2,3,6-tetrahydropyridin-4-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.27 (t, J=5.9 Hz, 1H), 8.50 (d, J=7.1 Hz,1H), 8.41 (s, 1H), 7.89 (s, 1H), 7.38-7.56 (m, 7H), 6.85 (dd, J=6.8, 1.7Hz, 1H), 6.56-6.89 (m, 1H), 4.49 (d, J=5.8 Hz, 2H), 4.08-4.40 (m, 2H),3.74-3.92 (m, 1H), 3.44-3.66 (m, 1H), 2.66 (s, 2H); MS (ESI(+)) m/e 444(M+H)⁺.

Example 2984-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamideExample 298A 4-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-bromobenzoic acid for 4-nitrobenzoic acid.

Example 298B4-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 51A,substituting1-(2-hydroxy-2-methylpropyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 4-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.05 (t, J=5.9 Hz, 1H),8.49 (dd, J=6.9, 0.9 Hz, 1H), 8.19 (d, J=0.8 Hz, 1H), 7.97 (d, J=0.7 Hz,1H), 7.95-7.86 (m, 3H), 7.73-7.66 (m, 2H), 7.52 (d, J=1.2 Hz, 1H),7.42-7.37 (m, 1H), 6.87 (dd, J=7.0, 1.7 Hz, 1H), 4.73 (s, 1H), 4.51 (d,J=5.8 Hz, 2H), 4.04 (s, 2H), 1.10 (s, 6H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 299N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-phenylthiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting 4,4,5,5-tetramethyl-2-phenyl-1,3,2-dioxaborolane for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.14 (t, J=6.0 Hz,1H), 8.50 (dd, J=7.1, 0.7 Hz, 1H), 7.91-7.88 (m, 1H), 7.84 (d, J=3.9 Hz,1H), 7.72 (dt, J=8.3, 2.4 Hz, 2H), 7.57 (d, J=3.9 Hz, 1H), 7.53 (d,J=1.2 Hz, 1H), 7.49-7.33 (m, 4H), 6.86 (dd, J=7.0, 1.7 Hz, 1H), 4.50 (d,J=5.8 Hz, 2H); MS (ESI(+)) m/e 334 (M+H).

Example 301 tert-butyl3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)pyrrolidin-3-yl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.06 (t, J=5.9 Hz,1H), 8.48 (dd, J=6.9, 0.9 Hz, 1H), 7.87 (m, 3H), 7.52 (d, J=1.2 Hz, 1H),7.40 (m, 3H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 4.50 (d, J=5.9 Hz, 2H), 3.72(dd, J=10.3, 7.5 Hz, 1H), 3.47 (m, 2H), 3.20 (m, 2H), 2.21 (m, 1H), 1.97(m, 1H), 1.41 (m, 9H); (ESI(+)) m/e 421 (M+H)⁺.

Example 302 tert-butyl3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 3-(4-aminophenyl)pyrrolidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.61(s, 1H), 8.48 (dd, J=6.9, 0.9 Hz, 1H), 7.88 (d, J=1.1 Hz, 1H), 7.51 (d,J=1.2 Hz, 1H), 7.36 (m, 3H), 7.14 (m, 2H), 6.83 (dd, J=7.0, 1.7 Hz, 1H),6.69 (t, J=6.0 Hz, 1H), 4.33 (d, J=6.0 Hz, 2H), 3.65 (dd, J=10.2, 7.5Hz, 1H), 3.46 (m, 1H), 3.21 (m, 2H), 3.09 (m, 1H), 2.12 (m, 1H), 1.89(m, 1H), 1.41 (m, 9H); (ESI(+)) m/e 436 (M+H)⁺.

Example 303N-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)biphenyl-2-sulfonamideExample 303A tert-butyl4-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)phenylcarbamate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-aminophenylcarbamate for 4-amino-N-isopentylbenzamide andimidazo[1,2-a]pyridin-7-ylmethanamine for imidazo[1,2-a]pyridin-6-amine.

Example 303B 1-(4-aminophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)phenylcarbamate fortert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 303CN-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)biphenyl-2-sulfonamide

In a 4 mL vial was mixed1-(4-aminophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea (50 mg, 0.178mmol) in anhydrous tetrahydrofuran (2 mL). To this mixture at roomtemperature was added 60% sodium hydride (24.88 mg, 0.622 mmol). Thereaction was stirred about 30 minutes and biphenyl-2-sulfonyl chloride(53.9 mg, 0.213 mmol) was added. The reaction mixture stirred overnightat room temperature and was quenched with saturated ammonium chlorideand water. The aqueous solution was extracted with dichloromethane and10% methanol/dichloromethane. The organic layers were combined,concentrated and purified by normal phase chromatography to give thetitle compound. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.74 (bs, 1H), 8.56 (s,1H), 8.47 (dd, J=6.9, 0.9 Hz, 1H), 7.95 (dd, J=7.8, 1.4 Hz, 1H), 7.87(dd, J=1.2, 0.6 Hz, 1H), 7.62 (m, 1H), 7.54 (m, 1H), 7.51 (m, 1H), 7.38(m, 4H), 7.30-7.20 (m, 5H), 6.82 (m, 3H), 6.66 (t, J=6.0 Hz, 1H), 4.30(d, J=6.0 Hz, 2H); (ESI(+)) m/e 498 (M+H)⁺.

Example 3061-{2-fluoro-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureaExample 306A1-(2-fluoro-4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 306B1-{2-fluoro-4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(2-fluoro-4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, methanol-d₄) δ ppm 8.74 (d, J=7.0 Hz, 1H), 8.19-8.15(m, 1H), 8.00-7.96 (m, 1H), 7.92 (t, J=8.5 Hz, 1H), 7.81-7.77 (m, 1H),7.50-7.44 (m, 1H), 7.28-7.16 (m, 2H), 6.17-6.11 (m, 1H), 4.61 (bs, 2H),4.30-4.15 (m, 2H), 3.79 (t, J=5.7 Hz, 2H), 3.08-2.90 (m, 1H), 2.62-2.45(m, 2H), 1.17-1.08 (m, 6H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 3071-{2-fluoro-4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(2-fluoro-4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 3-methylbutan-1-amine and tetrahydrofuran-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, methanol-d₄) δ ppm 8.74 (d, J=7.0Hz, 1H), 8.17 (d, J=2.2 Hz, 1H), 7.98 (d, J=2.2 Hz, 1H), 7.92 (t, J=8.5Hz, 1H), 7.80 (bs, 1H), 7.47 (dd, J=7.0, 1.5 Hz, 1H), 7.28-7.16 (m, 2H),6.17-6.09 (m, 1H), 4.84-4.70 (m, 1H), 4.61 (bs, 2H), 4.34-4.12 (m, 2H),4.01-3.68 (m, 4H), 2.67-2.47 (m, 2H), 2.29-1.88 (m, 4H); MS (ESI(+)) m/e464 (M+H)⁺.

Example 314 tert-butyl4-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate Example 314A2-(4-bromophenyl)-N-(imidazo[1,2-a]pyridin-6-yl)acetamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-amine for 3-methylbutan-1-amine and2-(4-bromophenyl)acetic acid for 4-nitrobenzoic acid.

Example 314B tert-butyl4-{4-[2-(imidazo[1,2-a]pyridin-6-ylamino)-2-oxoethyl]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 2-(4-bromophenyl)-N-(imidazo[1,2-a]pyridin-6-yl)acetamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.25 (s, 1H), 9.20-9.16(m, 1H), 7.98-7.94 (m, 1H), 7.58-7.48 (m, 2H), 7.44-7.36 (m, 2H),7.35-7.28 (m, 2H), 7.16 (dd, J=9.6, 2.0 Hz, 1H), 6.16-6.09 (m, 1H),4.05-3.94 (m, 2H), 3.66 (s, 2H), 3.53 (t, J=5.7 Hz, 2H), 2.49-2.40 (m,2H), 1.42 (s, 9H); MS (ESI(+)) m/e 433 (M+H)⁺.

Example 315N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]benzamide

The title compound was prepared as described in Example 51A,substituting 4-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04 (t, J=5.9 Hz, 1H),8.49 (dd, J=7.0, 0.9 Hz, 1H), 8.27 (s, 1H), 8.00-7.86 (m, 4H), 7.69 (d,J=8.4 Hz, 2H), 7.52 (d, J=1.2 Hz, 1H), 7.40 (d, J=1.5 Hz, 1H), 6.87 (dd,J=7.0, 1.7 Hz, 1H), 4.51 (d, J=5.9 Hz, 2H), 3.94 (d, J=7.1 Hz, 2H), 2.15(dp, J=13.6, 6.8 Hz, 1H), 0.87 (d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 374(M+H)⁺.

Example 318N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(propan-2-yloxy)phenyl]thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting2-(3-isopropoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04 (t, J=6.0 Hz,1H), 8.49 (dd, J=7.0, 0.8 Hz, 1H), 8.19 (d, J=0.4 Hz, 1H), 7.89 (d,J=0.8 Hz, 1H), 7.86 (d, J=0.5 Hz, 1H), 7.75 (d, J=3.9 Hz, 1H), 7.52 (d,J=1.2 Hz, 1H), 7.40 (s, 1H), 7.24 (d, J=3.9 Hz, 1H), 6.85 (dd, J=7.0,1.7 Hz, 1H), 4.48 (d, J=5.8 Hz, 2H), 4.13 (d, J=6.6 Hz, 2H), 3.09-2.83(m, 4H), 2.47-2.40 (m, 1H), 2.14-1.96 (m, 1H), 1.88-1.69 (m, 1H),1.69-1.54 (m, 1H), 1.37-1.14 (m, 1H).

Example 319N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1,2,3,6-tetrahydropyridin-4-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and tetrahydro-2H-pyran-4-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.26 (t, J=5.9 Hz,1H), 8.50 (d, J=6.8 Hz, 1H), 8.40 (s, 1H), 7.89 (s, 1H), 7.52 (d, J=1.4Hz, 1H), 7.42 (s, 1H), 6.84 (dd, J=7.1, 1.7 Hz, 1H), 6.72-6.79 (m, 1H),4.49 (d, J=5.8 Hz, 2H), 4.32 (s, 1H), 4.16 (s, 1H), 3.81-3.89 (m, 2H),3.73 (s, 2H), 3.36-3.47 (m, 1H), 2.83-3.05 (m, 1H), 2.65 (s, 1H),2.38-2.54 (m, 2H), 1.50-1.69 (m, 4H); MS (ESI(+)) m/e 452 (M+H)⁺.

Example 320N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1,2,3,6-tetrahydropyridin-4-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.26 (t, J=5.9 Hz, 1H), 8.50 (d, J=7.1Hz, 1H), 8.40 (s, 1H), 7.89 (s, 1H), 7.53 (s, 1H), 7.42 (s, 1H), 6.84(dd, J=7.1, 1.7 Hz, 1H), 6.76 (s, 1H), 4.49 (d, J=5.8 Hz, 2H), 4.29 (s,1H), 4.16 (s, 1H), 3.62-3.74 (m, 2H), 2.81-3.03 (m, 1H), 2.60-2.69 (m,1H), 2.50-2.58 (m, 1H), 1.02 (d, J=6.4 Hz, 6H); MS (ESI(+)) m/e 410(M+H)⁺.

Example 321N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamideExample 321A (S)-tert-butyl3-(4-(benzyloxycarbonyl)phenoxy)pyrrolidine-1-carboxylate

To a stirred solution of (R)-tert-butyl3-hydroxypyrrolidine-1-carboxylate (1 g, 5.34 mmol) in tetrahydrofuran(38.1 ml) was added benzyl 4-hydroxybenzoate (1.341 g, 5.87 mmol) andtriphenylphosphine polymer bound (4.45 g, 8.01 mmol). The reactionmixture was cooled to 0° C. and a solution of (E)-diisopropyldiazene-1,2-dicarboxylate (1.367 ml, 6.94 mmol) in tetrahydrofuran (5mL) was added dropwise over 15 minutes. The reaction was allowed to stirat room temperature for 16 hours and the mixture was filtered. Thesolids were washed with dichloromethane, and the combined filtrates wereconcentrated and purified by normal phase chromatography to give thetitle compound.

Example 321B (S)-4-(1-(tert-butoxycarbonyl)pyrrolidin-3-yloxy)benzoicacid

The title compound was prepared as described in Example 1B, substituting(R)-tert-butyl 3-(4-(benzyloxycarbonyl)phenoxy)pyrrolidine-1-carboxylatefor N-isopentyl-4-nitrobenzamide.

Example 321C (S)-tert-butyl3-(4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)phenoxy)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and(S)-4-(1-(tert-butoxycarbonyl)pyrrolidin-3-yloxy)benzoic acid for4-nitrobenzoic acid.

Example 321D(S)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamide

The title compound was prepared as described in Example 28A,substituting (S)-tert-butyl3-(4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)phenoxy)pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 321EN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide

The title compound was prepared as described in Example 1A, substituting(S)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamidefor 3-methylbutan-1-amine and (S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm8.67-8.59 (m, 1H), 8.41 (d, J=6.9 Hz, 1H), 7.90-7.84 (m, 2H), 7.81 (s,1H), 7.50-7.46 (m, 1H), 7.38 (s, 1H), 7.03-6.97 (m, 2H), 6.83 (dd,J=6.9, 1.7 Hz, 1H), 5.17-5.04 (m, 1H), 4.49 (d, J=5.9 Hz, 2H), 3.91-3.36(m, 5H), 2.31-1.98 (m, 2H), 1.63-1.49 (m, 1H), 1.38-1.23 (m, 1H), 1.00(d, J=6.7 Hz, 3H), 0.89-0.74 (m, 3H); MS (ESI(+)) m/e 421 (M+H)⁺.

TABLE 16 The following Examples were prepared essentially as describedin Example 321, substituting the appropriate carboxylic acid in Example321E. Ex Name MS 339N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3R)- (ESI(+))tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide m/e 435 (M +H)⁺ 340 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2R)- (ESI(+))tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide m/e 435 (M +H)⁺ 341 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(2S)- (ESI(+))tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide m/e 435 (M +H)⁺ 342 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-(ESI(+)) pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}benzamide m/e 449 (M +H)⁺ 343 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(tetrahydro-2H-(ESI(+)) pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}benzamide m/e 463 (M + H)⁺346 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3S)-1-[(3S)- (ESI(+))tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide m/e 435 (M +H)⁺ 347 4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 419 (M + H)⁺ 3484-{[(3S)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-yl]oxy}- (ESI(+))N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 423 (M + H)⁺ 349N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(3-methoxy-2- (ESI(+))methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide m/e 437 (M + H)⁺ 3504-{[(3S)-1-butanoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 407 (M + H)⁺ 351N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3S)-1-(2- (ESI(+))methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide m/e 407 (M + H)⁺ 3524-{[(3S)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 405 (M + H)⁺ 3534-{[(3S)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 441 (M + H)⁺ 3544-{[(3S)-1-(3-hydroxy-3-methylbutanoyl)pyrrolidin-3-yl]oxy}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide m/e 437 (M + H)⁺

Example 322 tert-butyl4-[4-(imidazo[1,2-a]pyridin-7-ylcarbamoyl)phenyl]piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-amine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.36 (s, 1H), 8.47 (d, J=7.3 Hz,1H), 8.15-8.10 (m, 1H), 7.94-7.87 (m, 2H), 7.83 (s, 1H), 7.50-7.40 (m,3H), 7.24 (dd, J=7.3, 2.1 Hz, 1H), 4.16-4.05 (m, 2H), 2.94-2.66 (m, 3H),1.84-1.73 (m, 2H), 1.65-1.41 (m, 11H); MS (ESI(+)) m/e 421 (M+H)⁺.

Example 323 tert-butyl4-[4-(imidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl]piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-amine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.27 (s, 1H), 9.36-9.31 (m, 1H),8.03 (s, 1H), 7.95-7.88 (m, 2H), 7.60-7.52 (m, 2H), 7.47-7.35 (m, 3H),4.15-4.04 (m, 2H), 2.95-2.66 (m, 3H), 1.83-1.73 (m, 2H), 1.65-1.45 (m,2H), 1.42 (s, 9H); MS (ESI(+)) m/e 421 (M+H)⁺.

Example 324N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(2-methylpropanoyl)amino]oxetan-3-yl}thiophene-2-carboxamideExample 324A5-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)thiophene-2-carboxylicacid

Butyllithium (6.16 ml, 15.41 mmol) was added dropwise to a stirredsolution of diisopropylamine (1.919 ml, 13.69 mmol) in tetrahydrofuran(10 ml) at −78° C. The solution was allowed to warm to room temperatureand then added dropwise by syringe to a stirred −78° C. solution ofthiophene-2-carboxylic acid (0.877 g, 6.85 mmol) in tetrahydrofuran (30ml). The resulting suspension was stirred for 40 minutes at −78° C. whena solution of 2-methyl-N-(oxetan-3-ylidene)propane-2-sulfinamide (1 g,5.71 mmol) in tetrahydrofuran (10 ml) was added dropwise. After theaddition was complete, the reaction mixture was allowed to warm to roomtemperature, quenched with saturated ammonium chloride and diluted witha water to dissolve the remaining solids. The aqueous solution wasextracted with ethyl acetate, adjusted to pH 2 by addition of 1N aqueoushydrochloric acid and re-extracted with ethyl acetate and methylenechloride. The organic extracts were dried with magnesium sulfate,filtered, concentrated and purified by normal phase chromatography togive the title compound.

Example 324B5-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)thiophene-2-carboxylicacid for 4-nitrobenzoic acid.

Example 324C5-(3-aminooxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

5-(3-(1,1-Dimethylethylsulfinamido)oxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide(432 mg, 1 mmol) in 10 ml methanol was treated with 4N aqueous HCl indioxane (0.75 ml, 3 mmol) and the mixture was stirred for 2 hours.Concentration provided the title compound.

Example 324D

The title compound was prepared as described in Example 1A, substituting5-(3-aminooxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03-9.10 (m, 2H), 8.48 (d, J=7.1 Hz,1H), 7.89 (s, 1H), 7.71 (d, J=4.0 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.38(s, 1H), 7.22 (d, J=4.0 Hz, 1H), 6.83 (dd, J=6.9, 1.8 Hz, 1H), 4.80 (d,J=6.7 Hz, 2H), 4.71 (d, J=6.7 Hz, 2H), 4.46 (d, J=6.0 Hz, 2H), 2.40-2.48(m, 1H), 1.05 (d, J=7.1 Hz, 6H); MS (ESI(+)) m/e 399 (M+H)⁺.

Example 3255-[3-(benzoylamino)oxetan-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-aminooxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, 1H), 9.05 (t, J=5.9 Hz, 1H), 8.47(d, J=6.8 Hz, 1H), 7.87-7.93 (m, 3H), 7.72 (d, J=3.7 Hz, 1H), 7.56-7.62(m, 1H), 7.48-7.55 (m, 3H), 7.37 (s, 1H), 7.29 (d, J=3.7 Hz, 1H), 6.82(dd, J=7.1, 1.7 Hz, 1H), 5.01 (d, J=6.8 Hz, 2H), 4.80 (d, J=7.1 Hz, 2H),4.45 (d, J=5.8 Hz, 2H); MS (ESI(+)) m/e 433 (M+H)⁺.

Example 326N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{3-[(tetrahydrofuran-3-ylacetyl)amino]oxetan-3-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-aminooxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 2-(tetrahydrofuran-3-yl)acetic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.22 (s, 1H), 9.07(t, J=6.0 Hz, 1H), 8.48 (d, J=7.1 Hz, 1H), 7.89 (s, 1H), 7.71 (d, J=3.6Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.38 (s, 1H), 7.22 (d, J=4.0 Hz, 1H),6.83 (dd, J=7.1, 1.6 Hz, 1H), 4.81 (d, J=6.7 Hz, 2H), 4.72 (d, J=6.7 Hz,2H), 4.46 (d, J=6.0 Hz, 2H), 3.56-3.80 (m, 3H), 2.23-2.30 (m, 2H),1.89-2.04 (m, 1H), 1.45-1.58 (m, 1H); MS (ESI(+)) m/e 441 (M+H)⁺.

Example 327N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[3-(pentanoylamino)oxetan-3-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-aminooxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and pentanoic acid for 4-nitrobenzoic acid. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.11 (s, 1H), 9.05 (t, J=5.9 Hz, 1H), 8.48(dd, J=7.0, 0.8 Hz, 1H), 7.88 (s, 1H), 7.70 (d, J=4.1 Hz, 1H), 7.52 (d,J=1.4 Hz, 1H), 7.38 (s, 1H), 7.21 (d, J=3.7 Hz, 1H), 6.83 (dd, J=7.1,1.7 Hz, 1H), 4.80 (d, J=6.8 Hz, 2H), 4.71 (d, J=6.8 Hz, 2H), 4.46 (d,J=5.8 Hz, 2H), 2.17 (t, J=7.5 Hz, 2H), 1.44-1.57 (m, 2H), 1.22-1.37 (m,2H), 0.84-0.92 (m, 3H); MS (ESI(+)) m/e 413 (M+H)⁺.

Example 3281-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)phenyl]ureaExample 328A (R)-tert-butyl 3-(4-nitrophenoxy)pyrrolidine-1-carboxylate

(R)-Tert-butyl 3-hydroxypyrrolidine-1-carboxylate (10 g, 53.4 mmol) wasdissolved in 1-fluoro-4-nitrobenzene (13.94 g, 99 mmol). An aqueoussolution of 5.9N potassium hydroxide (77 ml, 452 mmol) was addedfollowed by addition of tetrabutylammonium bromide (2.238 g, 6.94 mmol).The reaction mixture was stirred at 40° C. for 24 hours, cooled, dilutedwith water and extracted with ethyl acetate. The combined organic layerswere dried with sodium sulfate, filtered and concentrated to give thetitle compound.

Example 328B (R)-tert-butyl 3-(4-aminophenoxy)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1B, substituting(R)-tert-butyl 3-(4-nitrophenoxy)pyrrolidine-1-carboxylate forN-isopentyl-4-nitrobenzamide.

Example 328C tert-butyl(3S)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1C, substituting(R)-tert-butyl 3-(4-aminophenoxy)pyrrolidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine.

Example 328D(R)-1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(pyrrolidin-3-yloxy)phenyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl(3S)-3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 328E1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3S)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)phenyl]urea

The title compound was prepared as described in Example 1A, substituting(R)-1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(pyrrolidin-3-yloxy)phenyl)ureafor 3-methylbutan-1-amine and (S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.76-8.70 (m,1H), 8.19-8.12 (m, 1H), 8.00-7.94 (m, 1H), 7.81-7.75 (m, 1H), 7.46 (d,J=7.0 Hz, 1H), 7.34-7.25 (m, 2H), 6.92-6.82 (m, 2H), 5.07-4.95 (m, 1H),4.58 (bs, 2H), 3.84-3.61 (m, 3H), 3.60-3.45 (m, 1H), 2.67-2.45 (m, 1H),2.31-2.06 (m, 2H), 1.72-1.57 (m, 1H), 1.50-1.35 (m, 1H), 1.12-1.00 (m,3H), 0.94-0.85 (m, 3H); MS (ESI(+)) m/e 436 (M+H)⁺.

TABLE 17 The following Examples were prepared essentially as describedin Example 328, substituting the appropriate alcohol in Example 328A andthe appropriate carboxylic acid in Example 328E. Ex Name MS 3291-(4-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}phenyl)-3-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)urea m/e 456 (M + H)⁺ 3301-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(2- (ESI(+))methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)urea m/e 422 (M + H)⁺ 3311-(4-{[(3R)-1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-3-(ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 420 (M + H)⁺ 3321-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 434 (M + H)⁺ 3331-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-(ESI(+)) pyran-4-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)urea m/e 464 (M +H)⁺ 334 1-(4-{[(3R)-1-(2-hydroxy-2-methylpropanoyl)pyrrolidin-3-(ESI(+)) yl]oxy}phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 438(M + H)⁺ 335 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2R)-(ESI(+)) tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]uream/e 450 (M + H)⁺ 3361-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[(2S)- (ESI(+))tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]urea m/e 450(M + H)⁺ 337 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(ESI(+)) (tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)uream/e 450 (M + H)⁺ 3381-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[(3R)-1-(tetrahydro-2H-(ESI(+)) pyran-4-ylacetyl)pyrrolidin-3-yl]oxy}phenyl)urea m/e 478 (M +H)⁺ 689 1-(4-{[(3R)-1-(2-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 474 (M + H)⁺ 6901-(4-{[(3R)-1-(3-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 474 (M + H)⁺ 6911-(4-{[(3R)-1-(4-fluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 474 (M + H)⁺ 6921-(4-{[(3R)-1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 492 (M + H)⁺ 6931-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-({(3R)-1-[4- (ESI(+))(trifluoromethyl)benzoyl]pyrrolidin-3-yl}oxy)phenyl]urea m/e 524 (M +H)⁺ 6941-(4-{[(3R)-1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3-(ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 492 (M + H)⁺ 6951-(4-{[(3R)-1-(2-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 490 (M + H)⁺ 6961-(4-{[(3R)-1-(4-chlorobenzoyl)pyrrolidin-3-yl]oxy}phenyl)-3- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)urea m/e 490 (M + H)⁺

Example 3552-(4-benzoylpiperazin-1-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 53B, substitutingphenyl(piperazin-1-yl)methanone for 4-cyanobenzylamine and2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamide for2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide. ¹H NMR(300 MHz, DMSO-d₆) δ ppm 8.86 (t, J=6.0 Hz, 1H), 8.48 (d, J=6.7 Hz, 1H),7.90 (s, 1H), 7.89 (s, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.41-7.50 (m, 5H),7.37 (s, 1H), 6.82 (dd, J=7.1, 1.6 Hz, 1H), 4.43 (d, J=5.6 Hz, 2H),3.41-3.82 (m, 8H); MS (ESI(+)) m/e 447 (M+H)⁺.

Example 356N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(propan-2-yl)piperazin-1-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 53B, substituting1-isopropylpiperazine for 4-cyanobenzylamine and2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamide for2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide. ¹H NMR(300 MHz, DMSO-d₆) δ ppm 8.80 (t, J=5.9 Hz, 1H), 8.48 (d, J=7.1 Hz, 1H),7.88 (s, 1H), 7.87 (s, 1H), 7.52 (d, J=1.4 Hz, 1H), 7.37 (s, 1H), 6.81(dd, J=7.1, 1.7 Hz, 1H), 4.42 (d, J=6.1 Hz, 2H), 3.41-3.48 (m, 4H),2.64-2.79 (m, 1H), 2.51-2.57 (m, 4H), 0.98 (d, J=6.4 Hz, 6H); MS(ESI(+)) m/e 385 (M+H)⁺.

Example 357N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as in Example 53B, substituting1-(2-methoxyethyl)piperazine for 4-cyanobenzylamine and2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamide for2-bromo-N-(imidazo[1,2-a]pyridin-6-yl)thiazole-5-carboxamide. ¹H NMR(300 MHz, DMSO-d₆) δ ppm 8.82 (t, J=6.0 Hz, 1H), 8.48 (d, J=6.7 Hz, 1H),7.88 (s, 1H), 7.88 (s, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.37 (s, 1H), 6.81(dd, J=7.1, 1.6 Hz, 1H), 4.43 (d, J=6.0 Hz, 2H), 3.42-3.48 (m, 6H), 3.24(s, 3H), 2.51-2.56 (m, 6H); MS (ESI(+)) m/e 401 (M+H)⁺.

Example 358N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamideExample 358A methyl4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)benzoate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(methoxycarbonyl)benzoic acid for 4-nitrobenzoic acid.

Example 358B 4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)benzoic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)benzoate for methyl4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 358CN-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide

The title compound was prepared as described in Example 1A, substituting3-methylbutan-1-amine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.15 (t, J=5.8 Hz,1H), 8.55-8.47 (m, 2H), 8.00-7.84 (m, 5H), 7.54 (dd, J=5.1, 4.1 Hz, 2H),7.23 (dd, J=9.3, 1.7 Hz, 1H), 4.48 (d, J=5.8 Hz, 2H), 3.30-3.21 (m, 2H),1.62 (dp, J=13.3, 6.6 Hz, 1H), 1.49-1.37 (m, 2H), 0.91 (d, J=6.6 Hz,6H); MS (ESI(+)) m/e 365 (M+H)⁺.

Example 359N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide

The title compound was prepared as described in Example 1A, substituting(S)-(tetrahydrofuran-3-yl)methanamine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-6-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.15 (t, J=5.8 Hz,1H), 8.68 (t, J=5.7 Hz, 1H), 8.49 (bs, 1H), 8.03-7.85 (m, 5H), 7.58-7.50(m, 2H), 7.23 (dd, J=9.1, 1.7 Hz, 1H), 4.49 (d, J=5.8 Hz, 2H), 3.80-3.56(m, 4H), 3.48 (dd, J=8.5, 5.2 Hz, 1H), 3.28-3.17 (m, 1H), 2.03-1.87 (m,1H), 1.68-1.46 (m, 1H), 1.37-1.09 (m, 1H); MS (ESI(+)) m/e 379 (M+H)⁺.

Example 3601-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]ureaExample 360A 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-6-ylmethyl)urea

The title compound was prepared as described in Example 3A, substituting1-isocyanato-4-bromobenzene for 1-isocyanato-4-nitrobenzene andimidazo[1,2-a]pyridin-6-ylmethanamine for imidazo[1,2-a]pyridin-6-amine.

Example 360B1-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea

The title compound was prepared as described in Example 51A,substituting1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-6-ylmethyl)urea for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.44 (s,1H), 8.04 (s, 1H), 7.95 (s, 1H), 7.76 (s, 1H), 7.57-7.50 (m, 2H),7.48-7.32 (m, 4H), 7.21 (dd, J=9.2, 1.7 Hz, 1H), 6.65 (t, J=5.9 Hz, 1H),4.30 (d, J=5.8 Hz, 2H), 4.04 (t, J=6.9 Hz, 2H), 1.87-1.73 (m, 2H), 0.84(t, J=7.3 Hz, 3H); MS (ESI(+)) m/e 375 (M+H)⁺.

Example 361N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-phenyl-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 51A,substituting phenyl boronic acid for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.34 (t, J=5.8 Hz,1H), 8.56-8.48 (m, 2H), 8.05-7.95 (m, 2H), 7.90 (d, J=0.8 Hz, 1H),7.60-7.49 (m, 4H), 7.45 (s, 1H), 6.87 (dd, J=7.0, 1.6 Hz, 1H), 4.52 (d,J=5.7 Hz, 2H); MS (ESI(+)) m/e 335 (M+H).

Example 3621-(imidazo[1,2-a]pyridin-6-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea

The title compound was prepared as described in Example 51A,substituting 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-6-ylmethyl)ureafor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.44(d, J=1.6 Hz, 1H), 8.03 (d, J=0.8 Hz, 1H), 7.97-7.93 (m, 1H), 7.77 (d,J=0.8 Hz, 1H), 7.57-7.50 (m, 2H), 7.44-7.35 (m, 4H), 7.21 (dd, J=9.2,1.7 Hz, 1H), 6.65 (t, J=5.9 Hz, 1H), 4.30 (d, J=5.8 Hz, 2H), 3.90 (d,J=7.2 Hz, 2H), 2.19-2.06 (m, 1H), 0.85 (d, J=6.7 Hz, 6H); MS (ESI(+))m/e 389 (M+H)⁺.

Example 364 tert-butyl3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)azetidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 3-(4-aminophenyl)azetidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.66(s, 1H), 8.48 (m, 1H), 7.88 (s, 1H), 7.51 (d, J=1.2 Hz, 1H), 7.39 (m,3H), 7.19 (m, 2H), 6.83 (dd, J=7.0, 1.6 Hz, 1H), 6.70 (t, J=6.0 Hz, 1H),4.33 (d, J=6.0 Hz, 2H), 4.20 (m, 2H), 3.78 (m, 2H), 3.71 (m, 1H), 1.40(s, 9H); (ESI(+)) m/e 422 (M+H)⁺.

Example 365 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yloxy)benzoic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.95 (t, J=6.0 Hz,1H), 8.48 (dd, J=6.9, 0.9 Hz, 1H), 7.88 (m, 3H), 7.51 (d, J=1.2 Hz, 1H),7.37 (s, 1H), 7.06 (m, 2H), 6.85 (dd, J=7.0, 1.6 Hz, 1H), 4.67 (m, 1H),4.49 (d, J=5.9 Hz, 2H), 3.67 (m, 2H), 3.18 (m, 2H), 1.92 (m, 2H), 1.52(m, 2H), 1.41 (s, 9H); (ESI(+)) m/e 451 (M+H)⁺.

Example 366 tert-butyl4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminophenoxy)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.47(m, 2H), 7.88 (d, J=1.1 Hz, 1H), 7.51 (d, J=1.2 Hz, 1H), 7.37 (s, 1H),7.30 (m, 2H), 6.85 (m, 3H), 6.62 (t, J=6.0 Hz, 1H), 4.42 (m, 1H), 4.32(d, J=6.0 Hz, 2H), 3.64 (m, 2H), 3.15 (m, 2H), 1.86 (m, 2H), 1.51 (m,2H), 1.40 (s, 9H); (ESI(+)) m/e 466 (M+H)⁺.

Example 367N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]benzamideExample 367AN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 367BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)pyrrolidin-3-yl]benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamide for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.07 (m, 1H), 8.48 (d, J=7.0 Hz, 1H), 7.88(m, 3H), 7.51 (d, J=1.2 Hz, 1H), 7.42 (m, 3H), 6.85 (dd, J=7.0, 1.6 Hz,1H), 4.50 (d, J=5.9 Hz, 2H), 3.90-3.66 (m, 1H), 3.63-3.20 (m, 4H), 2.70(m, 1H), 2.38-2.18 (m, 1H), 2.10-1.90 (m, 1H), 1.01 (m, 6H); (ESI(+))m/e 391 (M+H)⁺.

TABLE 18 The following Examples were prepared essentially as describedin Example 367, substituting the appropriate carboxylic acid in Example367B. Ex Name ¹H NMR MS 368 N-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δppm 9.07 (ESI(+)) a]pyridin-7- (m, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.87(m, m/e 405 ylmethyl)-4-{1- 3H), 7.52 (d, J = 1.2 Hz, 1H), 7.41 (m, 3H),(M + H)⁺ [(2S)-2- 6.85 (dd, J = 7.0, 1.6 Hz, 1H), 4.50 (d, J = 5.9methylbutanoyl]pyrrolidin- Hz, 2H), 3.90-3.66 (m, 1H), 3.63-3.20 (m,3-yl}benzamide 4H), 2.51 (m, 1H), 2.38-2.18 (m, 1H), 2.10- 1.90 (m, 1H),1.57 (m, 1H), 1.34 (m, 1H), 1.01 (m, 3H), 0.86 (m, 3H) 369 4-[1- ¹H NMR(500 MHz, DMSO-d₆) δ ppm 9.07 (ESI(+)) (cyclopropylacetyl) (m, 1H), 8.48(d, J = 7.0 Hz, 1H), 7.88 (m, m/e 403 pyrrolidin-3-yl]-N- 3H), 7.52 (d,J = 1.2 Hz, 1H), 7.42 (m, 3H), (M + H)⁺ (imidazo[1,2- 6.85 (dd, J = 7.0,1.6 Hz, 1H), 4.50 (d, J = 5.9 a]pyridin-7- Hz, 2H), 3.88 (m, 1H), 3.61(m, 1H), 3.60- ylmethyl)benzamide 3.20 (m, 3H), 2.35-2.15 (m, 3H),2.10-1.88 (m, 1H), 1.99 (m, 1H), 0.44 (m, 2H), 0.12 (m, 2H) 370 4-(1- ¹HNMR (500 MHz, DMSO-d₆) δ ppm 9.07 (ESI(+)) benzoylpyrrolidin- (m, 1H),8.48 (t, J = 6.2 Hz, 1H), 7.88 (m, m/e 425 3-yl)-N- 3H), 7.55 (m, 2H),7.54-7.34 (m, 7H), 6.85 (M + H)⁺ (imidazo[1,2- (m, 1H), 4.50 (m, 2H),4.00 (m, 1H), 3.73 (m, a]pyridin-7- 1H), 3.65-3.40 (m, 3H), 2.38-2.22(m, 1H), ylmethyl)benzamide 2.15-1.94 (m, 1H) 371 N-(imidazo[1,2- ¹H NMR(500 MHz, DMSO-d₆) δ ppm 9.07 (ESI(+)) a]pyridin-7- (m, 1H), 8.48 (d, J= 7.0 Hz, 1H), 7.89 (m, m/e 421 ylmethyl)-4-{1- 3H), 7.52 (d, J = 1.2Hz, 1H), 7.41 (m, 3H), (M + H)⁺ [(propan-2- 6.85 (dd, J = 7.0, 1.6 Hz,1H), 4.51 (d, J = 5.9 yloxy)acetyl]pyrrolidin- Hz, 2H), 4.05 (d, J = 4.5Hz, 2H), 3.95-3.81 3-yl}benzamide (m, 1H), 3.70-3.55 (m, 2H), 3.55-3.20(m, 3H), 2.38-2.18 (m, 1H), 2.08-1.88 (m, 1H), 1.11 (m, 6H) 3724-[1-(2-hydroxy-2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.07 (ESI(+))methylpropanoyl)pyrrolidin- (t, J = 6.0 Hz, 1H), 8.48 (d, J = 7.0 Hz,1H), m/e 407 3-yl]-N- 7.88 (m, 3H), 7.52 (d, J = 1.2 Hz, 1H), 7.42 (M +H)⁺ (imidazo[1,2- (m, 2H), 7.38 (m, 1H), 6.85 (dd, J = 7.0, 1.6a]pyridin-7- Hz, 1H), 5.15 (m, 1H), 4.50 (d, J = 5.9 Hz,ylmethyl)benzamide 2H), 4.34 (m, 1H), 3.85-3.65 (m, 1H), 3.59 (m, 3H),2.35-2.10 (m, 1H), 2.05-1.86 (m, 1H), 1.30 (m, 6H);) 373 N-(imidazo[1,2-¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.07 (ESI(+)) a]pyridin-7- (m, 1H), 8.48(d, J = 7.0 Hz, 1H), 7.88 (m, m/e 419 ylmethyl)-4-{1- 3H), 7.52 (s, 1H),7.45-7.35 (m, 3H), 6.85 (M + H)⁺ [(2R)- (d, J = 7.1 Hz, 1H), 4.55 (m,1H), 4.50 (m, tetrahydrofuran-2- 2H), 4.10-3.93 (m, 1H), 3.90-3.65 (m,3H), ylcarbonyl]pyrrolidin- 3.65-3.20 (m, 3H) 2.37-2.19 (m, 1H), 2.10-3-yl}benzamide 1.76 (m, 5H) 374 N-(imidazo[1,2- ¹H NMR (500 MHz,DMSO-d₆) δ ppm 9.08 (ESI(+)) a]pyridin-7- (m, 1H), 8.48 (m, 1H), 7.88(m, 3H), 7.52 (s, m/e 419 ylmethyl)-4-{1- 1H), 7.45-7.37 (m, 3H), 6.85(dd, J = 7.0, (M + H)⁺ [(2S)- 1.6 Hz, 1H), 4.55 (m, 1H), 4.50 (m, 2H),4.10- tetrahydrofuran-2- 3.93 (m, 1H), 3.90-3.65 (m, 3H), 3.65-ylcarbonyl]pyrrolidin- 3.20 (m, 3H) 2.37-2.19 (m, 1H), 2.10-1.753-yl}benzamide (m, 5H) 375 N-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δppm 9.08 (ESI(+)) a]pyridin-7- (m, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.89(m, m/e 419 ylmethyl)-4-{1- 3H), 7.52 (s, 1H), 7.46 (m, 1H), 7.41 (m,1H), (M + H)⁺ [(3S)- 7.38 (m, 1H), 6.85 (d, J = 7.1 Hz, 1H), 4.51tetrahydrofuran-3- (m, 2H), 4.10-3.93 (m, 1H), 3.95-3.80 (m,ylcarbonyl]pyrrolidin- 2H), 3.65-3.20 (m, 6H), 2.36-2.20 (m, 1H),3-yl}benzamide 2.14-1.85 (m, 4H) 376 N-(imidazo[1,2- ¹H NMR (500 MHz,DMSO-d₆) δ ppm 9.07 (ESI(+)) a]pyridin-7- (m, 1H), 8.48 (d, J = 7.0 Hz,1H), 7.88 (m, m/e 433 ylmethyl)-4-[1- 3H), 7.51 (s, 1H), 7.45 (d, J =8.0 Hz, 1H), (M + H)⁺ (tetrahydro-2H- 7.41 (m, 2H), 6.85 (m, 1H), 4.51(d, J = 3.0 pyran-4- Hz, 2H), 3.88 (m, 3H), 3.75 (m, .55 (m, 2H),ylcarbonyl)pyrrolidin- 3.55-3.20 (m, 3H), 2.71 (m, 1H), 2.39-2.193-yl]benzamide (m, 1H), 2.10-1.85 (m, 1H), 1.59 (m, 4H) 3774-[1-(1,4-dioxan-2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.07 (ESI(+))ylcarbonyl)pyrrolidin- (m, 1H), 8.48 (d, J = 7.1 Hz, 1H), 7.89 (m, m/e435 3-yl]-N- 3H), 7.52 (s, 1H), 7.43 (m, 2H), 7.38 (s, 1H), (M + H)⁺(imidazo[1,2- 6.85 (d, J = 7.1 Hz, 1H), 4.51 (dd, J = 5.8, 2.9a]pyridin-7- Hz, 2H), 4.27 (m, 2H), 4.15-4.00 (m, 1H),ylmethyl)benzamide 3.90-3.70 (m, 4H), 3.70-3.20 (m, 5H); 2.39- 2.19 (m,1H), 2.15-1.88 (m, 1H) 378 N-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δppm 9.07 (ESI(+)) a]pyridin-7- (m, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88(m, m/e 447 ylmethyl)-4-[1- 3H), 7.52 (s, 1H), 7.42 (m, 2H), 7.38 (s,1H), (M + H)⁺ (tetrahydro-2H- 6.85 (d, J = 7.1 Hz, 1H), 4.51 (m, 2H),3.95 pyran-4- (m, 1H), 3.83 (m, 3H), 3.63 (m, 1H), 3.47 (m,ylacetyl)pyrrolidin- 2H), 3.45-3.20 (m, 2H), 2.38-2.15 (m, 3H),3-yl]benzamide 2.10-1.90 (m, 2H), 1.56 (m, 2H), 1.21 (m, 2H) 488N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 431 ylmethyl)-4-[1- (M + H)⁺(thiophen-2- ylcarbonyl)pyrrolidin- 3-yl]benzamide 562 4-[1-(4- (ESI(+))fluorobenzo- m/e 443 yl)pyrrolidin-3-yl]- (M + H)⁺ N-(imidazo[1,2-a]pyridin-7- ylmethyl)benzamide 580 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 403 ylmethyl)-4-{1-[(2- (M + H)⁺ methylcyclopropyl)carbonyl]pyrrolidin- 3-yl}benzamide 581 4-[1- (ESI(+))(cyclopentylacetyl)pyrrolidin- m/e 431 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 582 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 419 ylmethyl)-4-[1-(3- (M + H)⁺methylpentanoyl)pyrrolidin- 3-yl]benzamide 583 4-[1- (ESI(+))(cyclopentylcarbon- m/e 417 yl)pyrrolidin- (M + H)⁺3-yl]-N-(imidazo[1,2- a]pyridin-7- ylmethyl)benzamide 584N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 403 ylmethyl)-4-{1-[(1- (M +H)⁺ methylcyclopropyl) carbonyl]pyrrolidin- 3-yl}benzamide 5854-[1-(2,2- (ESI(+)) dimethylpropanoyl) m/e 405 pyrrolidin-3-yl]-N- (M +H)⁺ (imidazo[1,2- a]pyridin-7- ylmethyl)benzamide 586 N-(imidazo[1,2-(ESI(+)) a]pyridin-7- m/e 432 ylmethyl)-4-[1-(1,3- (M + H)⁺ thiazol-5-ylcarbonyl)pyrrolidin- 3-yl]benzamide 587 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 455 ylmethyl)-4-[1-(2- (M + H)⁺methoxybenzoyl)pyrrolidin- 3-yl]benzamide 588 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 432 ylmethyl)-4-[1-(1,3- (M + H)⁺ thiazol-4-ylcarbonyl)pyrrolidin- 3-yl]benzamide 589 4-[1-(2- (ESI(+))fluorobenzoyl)pyrrolidin- m/e 443 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 590 4-[1-(furan-2- (ESI(+))ylcarbonyl)pyrrolidin- m/e 415 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 591 4-[1-(3- (ESI(+))fluorobenzoyl)pyrrolidin- m/e 443 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 592 4-[1-(2,4- (ESI(+))difluorobenzoyl)pyrrolidin- m/e 461 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 593 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 429 ylmethyl)-4-{1-[(1- (M + H)⁺ methyl-1H-pyrazol-3-yl)carbonyl]pyrrolidin- 3-yl}benzamide 594 4-[1-(2- (ESI(+))chlorobenzoyl)pyrrolidin- m/e 459 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 595 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 439 ylmethyl)-4-[1-(2- (M + H)⁺methylbenzoyl)pyrrolidin- 3-yl]benzamide 596 4-[1-(4- (ESI(+))chlorobenzoyl)pyrrolidin- m/e 459 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 597 4-[1-(3- (ESI(+))chlorobenzoyl)pyrrolidin- m/e 459 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 598 4-[1-(2,2- (ESI(+))dimethylbutanoyl)pyrrolidin- m/e 419 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 599 4-[1-(3,5- (ESI(+))difluorobenzoyl)pyrrolidin- m/e 461 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 600 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 439 ylmethyl)-4-[1-(4- (M + H)⁺methylbenzoyl)pyrrolidin- 3-yl]benzamide 601 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 405 ylmethyl)-4-[1-(3- (M + H)⁺methylbutanoyl)pyrrolidin- 3-yl]benzamide 602 4-[1-(3,3- (ESI(+))dimethylbutanoyl)pyrrolidin- m/e 419 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 603 4-[1-(3- (ESI(+))cyanobenzoyl)pyrrolidin- m/e 450 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 604 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 455 ylmethyl)-4-[1-(3- (M + H)⁺methoxybenzoyl)pyrrolidin- 3-yl]benzamide 605 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 455 ylmethyl)-4-[1-(4- (M + H)⁺methoxybenzoyl)pyrrolidin- 3-yl]benzamide 606 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 428 ylmethyl)-4-{1-[(1- (M + H)⁺ methyl-1H-pyrrol-2-yl)carbonyl]pyrrolidin- 3-yl}benzamide 607 4-[1- (ESI(+))(cyclohexylacetyl)pyrrolidin- m/e 445 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 608 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 426 ylmethyl)-4-[1- (M + H)⁺ (pyridin-4-ylcarbonyl)pyrrolidin- 3-yl]benzamide 609 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 426 ylmethyl)-4-[1- (M + H)⁺ (pyridin-3-ylcarbonyl)pyrrolidin- 3-yl]benzamide 610 4-[1- (ESI(+))(cyclohexylcarbon- m/e 431 yl)pyrrolidin-3-yl]-N- (M + H)⁺ (imidazo[1,2-a]pyridin-7- ylmethyl)benzamide 611 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 426 ylmethyl)-4-[1- (M + H)⁺ (pyridin-2-ylcarbonyl)pyrrolidin- 3-yl]benzamide 612 4-[1-(furan-3- (ESI(+))ylcarbonyl)pyrrolidin- m/e 415 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 613 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 432 ylmethyl)-4-[1-(1,3- (M + H)⁺ thiazol-2-ylcarbonyl)pyrrolidin- 3-yl]benzamide 614 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 445 ylmethyl)-4-{1-[(1- (M + H)⁺ methylcyclohexyl)car-bonyl]pyrrolidin- 3-yl}benzamide 615 4-[1-(2,3- (ESI(+))dimethylbutanoyl)pyrrolidin- m/e 419 3-yl]-N-(imidazo[1,2- (M + H)⁺a]pyridin-7- ylmethyl)benzamide 616 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 439 ylmethyl)-4-[1-(3- (M + H)⁺methylbenzoyl)pyrrolidin- 3-yl]benzamide 617 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 431 ylmethyl)-4-[1- (M + H)⁺ (thiophen-3-ylcarbonyl)pyrrolidin- 3-yl]benzamide 618 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 509 ylmethyl)-4-{1-[3- (M + H)⁺ (trifluorome-thoxy)benzoyl]pyrrolidin- 3-yl}benzamide 619 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 445 ylmethyl)-4-{1-[(3- (M + H)⁺ methylthiophen-2-yl)carbonyl]pyrrolidin- 3-yl}benzamide 620 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 493 ylmethyl)-4-{1-[3- (M + H)⁺ (trifluorometh-yl)benzoyl]pyrrolidin- 3-yl}benzamide 731 N-(imidazo[1,2- (ESI(+))a]pyridin-7- m/e 439 ylmethyl)-4-[1- (M + H)⁺ (phenylacetyl)pyrrolidin-3-yl]benzamide 732 N-(imidazo[1,2- (ESI(+)) a]pyridin-7- m/e 467ylmethyl)-4-[1-(2- (M + H)⁺ methyl-2- phenylpropanoyl)pyrrolidin-3-yl]benzamide 733 4-{1- (ESI(+)) [difluoro(phenyl)ace- m/e 475tyl]pyrrolidin-3-yl}- (M + H)⁺ N-(imidazo[1,2- a]pyridin-7-ylmethyl)benzamide

Example 3791-[4-(1-acetylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureaExample 379A1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(pyrrolidin-3-yl)phenyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl3-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 379B1-[4-(1-acetylpyrrolidin-3-yl)phenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(pyrrolidin-3-yl)phenyl)ureafor 3-methylbutan-1-amine and acetic acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, DMSO-d₆) δ ppm 8.62 (d, J=6.4 Hz, 1H), 8.48 (d, J=7.0 Hz,1H), 7.88 (s, 1H), 7.51 (s, 1H), 7.37 (m, 3H), 7.16 (m, 2H), 6.83 (dd,J=7.0, 1.6 Hz, 1H), 6.69 (m, 1H), 4.33 (d, J=6.0 Hz, 2H), 3.89-3.73 (m,1H), 3.65-3.45 (m, 3H), 3.10 (m, 1H), 2.29-2.11 (m, 1H), 2.00-1.80 (m,1H), 1.91 (s, 3H); (ESI(+)) m/e 378 (M+H)⁺.

Table 19

The following Examples were prepared essentially as described in Example379, substituting the appropriate carboxylic acid in Example 379B.

Ex Name ¹H NMR MS 380 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm8.62 (d, (ESI(+)) a]pyridin-7- J = 6.5 Hz, 1H), 8.48 (d, J = 7.0 Hz,1H), 7.88 m/e 406 ylmethyl)-3-{4- (s, 1H), 7.51 (s, 1H), 7.36 (m, 3H),7.16 (m, (M + H)⁺ [1-(2- 2H), 6.83 (d, J = 7.1 Hz, 1H), 6.70 (m, 1H),methylpropanoyl) 4.33 (d, J = 6.0 Hz, 2H), 3.80-3.65 (m, 1H),pyrrolidin-3- 3.60-3.48 (m, 1H), 3.45-3.20 (m, 2H), 3.13 yl]phenyl}urea(m, 1H), 2.68 (m, 1H), 2.30-2.10 (m, 1H), 2.05-1.80 (m, 1H), 1.00 (m,6H) 381 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.62 (d,(ESI(+)) a]pyridin-7- J = 6.5 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88m/e 420 ylmethyl)-3-(4- (s, 1H), 7.52 (s, 1H), 7.37 (m, 3H), 7.17 (m,(M + H)⁺ {1-[(2S)-2- 2H), 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.69 (t, J =methylbutanoyl]pyrro- 6.0 Hz, 1H), 4.33 (d, J = 6.0 Hz, 2H), 3.95-lidin-3- 3.75 (m, 1H), 3.70-3.45 (m, 2H), 3.45-3.20 yl}phenyl)urea (m,1H), 3.20 (m, 1H), 2.30-2.11 (m, 1H), 2.05-1.80 (m, 1H), 1.55 (m, 1H),1.25 (m, 2H), 0.96 (m, 3H), 0.87 (m, 3H) 382 1-{4-[1- - ¹H NMR (500 MHz,DMSO-d₆) δ ppm 8.62 (ESI(+)) (cyclopropyl- (d, J = 4.1 Hz, 1H), 8.49 (d,J = 7.0 Hz, 1H), m/e 418 acetyl)pyrrolidin-3- 7.89 (s, 1H), 7.52 (s,1H), 7.37 (m, 3H), 7.16 (M + H)⁺ yl]phenyl}-3- (m, 2H), 6.84 (d, J = 7.1Hz, 1H), 6.69 (t, J = (imidazo[1,2- 6.0 Hz, 1H), 4.33 (d, J = 6.0 Hz,2H), 3.80 (m, a]pyridin-7- 1H), 3.58 (m, 1H), 3.45 (m, 1H), 3.40-3.20ylmethyl)urea (m, 1H), 3.12 (m, 1H), 2.27-2.11 (m, 3H), 1.99-1.81 (m,1H), 0.98 (m, 1H), 0.44 (m, 2H), 0.11 (m, 2H) 383 1-[4-(1- ¹H NMR (500MHz, DMSO-d₆) δ ppm 8.62 (m, (ESI(+)) benzoylpyrrolidin- 1H), 8.48 (d, J= 6.1 Hz, 1H), 7.88 (d, J = 3.0 m/e 440 3-yl)phenyl]-3- Hz, 1H), 7.53(m, 3H), 7.50-7.35 (m, 5H), (M + H)⁺ (imidazo[1,2- 7.34 (d, 1H), 7.20(d, J = 8.2 Hz, 1H), 7.13 (d, J = a]pyridin-7- 8.2 Hz, 1H), 6.83 (m,1H), 6.68 (m, 1H), 4.33 ylmethyl)urea (d, J = 14.1 Hz, 2H), 3.68 (m,1H), 3.60-3.45 (m, 2H), 3.40-3.20 (m, 2H), 2.29-2.13 (m, 1H) 2.07-1.90(m, 1H) 384 1-(imidazo[1,2- - ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.63(ESI(+)) a]pyridin-7- (d, J = 6.0 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H), m/e436 ylmethyl)-3-(4- 7.88 (s, 1H), 7.51 (s, 1H), 7.37 (m, 3H), 7.16 (M +H)⁺ {1-[(propan-2- (m, 2H), 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.70 (m,yloxy)acetyl]pyrro- 1H), 4.33 (d, J = 6.0 Hz, 2H), 4.03 (d, J = 5.4lidin-3- Hz, 2H), 3.90-3.74 (m, 1H), 3.68-3.52 (m, yl}phenyl)urea 2H),3.47 (m, 1H), 3.40-3.20 (m, 1H), 3.16 (m, 1H), 2.29-2.11 (m, 1H),2.00-1.73 (m, 1H), 1.10 (m, 6H) 385 1-{4-[1-(2- ¹H NMR (500 MHz,DMSO-d₆) δ ppm 8.65 (d, (ESI(+)) hydroxy-2- J = 6.0 Hz, 1H), 8.48 (d, J= 7.0 Hz, 1H), 7.88 m/e 422 methylpropanoyl) (s, 1H), 7.51 (s, 1H), 7.37(m, 3H), 7.16 (m, (M + H)⁺ pyrrolidin-3- 2H), 6.83 (dd, J = 7.0, 1.6 Hz,1H), 6.73 (m, yl]phenyl}-3- 1H), 5.18 (bs, 1H), 4.33 (d, J = 6.0 Hz,2H), (imidazo[1,2- 4.28 (m, 1H), 3.80-3.60 (m, 1H), 3.60-3.10a]pyridin-7- (m, 3H), 2.25-2.08 (m, 1H), 1.97-1.73 (m, ylmethyl)urea1H), 1.30 (m, 6H) 386 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm8.62 (d, (ESI(+)) a]pyridin-7- J = 5.7 Hz, 1H), 8.48 (d, J = 7.0 Hz,1H), 7.88 m/e 434 ylmethyl)-3-(4- (s, 1H), 7.51 (s, 1H), 7.37 (m, 3H),7.16 (m, (M + H)⁺ {1-[(2R)- 2H), 6.83 (d, J = 6.2 Hz, 1H), 6.69 (t, J =6.0 tetrahydrofuran-2- Hz, 1H), 4.53 (m, 1H), 4.33 (d, J = 6.0 Hz, 2H),ylcarbonyl]pyrro- 3.85-3.64 (m, 3H), 3.63-3.45 (m, 1H), 3.45- lidin-3-3.20 (m, 2H), 3.16 (m, 1H), 2.29-2.10 (m, yl}phenyl)urea 1H), 2.08-1.92(m, 2H), 1.91-1.73 (m, 3H) 387 1-(imidazo[1,2- - ¹H NMR (500 MHz,DMSO-d₆) δ ppm 8.62 (ESI(+)) a]pyridin-7- (d, J = 5.6 Hz, 1H), 8.48 (d,J = 7.0 Hz, 1H), m/e 434 ylmethyl)-3-(4- 7.88 (s, 1H), 7.51 (s, 1H),7.36 (m, 3H), 7.16 (M + H)⁺ {1-[(2S)- (m, 2H), 6.83 (dd, J = 7.0, 1.6Hz, 1H), 6.69 (t, tetrahydrofuran-2- J = 6.0 Hz, 1H), 4.53 (m, 1H), 4.33(d, J = 6.0 ylcarbonyl]pyrro- Hz, 2H), 3.84-3.64 (m, 3H), 3.63-3.45 (m,lidin-3- 1H), 3.45-3.20 (m, 2H), 3.16 (m, 1H), 2.29- yl}phenyl)urea 2.10(m, 1H), 2.05-1.85 (m, 5H) 388 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆)δ ppm 8.63 (d, (ESI(+)) a]pyridin-7- J = 6.7 Hz, 1H), 8.48 (d, J = 7.0Hz, 1H), 7.88 m/e 434 ylmethyl)-3-(4- (s, 1H), 7.52 (s, 1H), 7.37 (m,3H), 7.17 (m, (M + H)⁺ {1-[(3S)- 2H), 6.83 (dd, J = 7.0, 1.6 Hz, 1H),6.70 (m, tetrahydrofuran-3- 1H), 4.33 (d, J = 6.0 Hz, 2H), 3.97-3.84 (m,ylcarbonyl]pyrro- 2H), 3.80-3.63 (m, 4H), 3.62-3.46 (m, 1H), lidin-3-3.45-3.10 (m, 3H), 2.29-2.10 (m, 1H), 2.09- yl}phenyl)urea 1.83 (m, 3H)389 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.62 (d, (ESI(+))a]pyridin-7- J = 7.5 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 m/e 448ylmethyl)-3-{4- (s, 1H), 7.51 (s, 1H), 7.36 (m, 3H), 7.16 (m, (M + H)⁺[1-(tetrahydro- 2H), 6.83 (d, J = 7.1 Hz, 1H), 6.69 (t, J = 6.02H-pyran-4- Hz, 1H), 4.33 (d, J = 6.0 Hz, 2H), 3.90-3.70ylcarbonyl)pyrro- (m, 3H), 3.55 (m, 1H), 3.45-3.20 (m, 3H), lidin-3-3.15 (m, 1H), 2.70 (m, 1H), 2.28-2.11 (m, yl]phenyl}urea 1H), 2.00-1.82(m, 1H), 1.57 (m, 4H) 390 1-{4-[1-(1,4- ¹H NMR (500 MHz, DMSO-d₆) δ ppm8.62 (d, (ESI(+)) dioxan-2- J = 7.5 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H),7.88 m/e 450 ylcarbonyl)pyrro- (s, 1H), 7.51 (s, 1H), 7.37 (m, 3H), 7.16(m, (M + H)⁺ lidin-3-yl]phenyl}- 2H), 6.83 (d, J = 7.1 Hz, 1H), 6.70 (t,J = 6.0 3-(imidazo[1,2- Hz, 1H), 4.33 (d, J = 6.0 Hz, 2H), 4.25 (m, 1H),a]pyridin-7- 3.85-3.70 (m, 3H), 3.70-3.60 (m, 2H), 3.60- ylmethyl)urea3.45 (m, 3H), 3.45-3.15 (m, 3H), 2.28-2.11 (m, 1H), 2.00-1.80 (m, 1H)391 1-(imidazo[1,2- - ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.62 (ESI(+))a]pyridin-7- (d, J = 5.5 Hz, 1H), 8.48 (d, J = 7.0 Hz, 1H), m/e 462ylmethyl)-3-{4- 7.88 (s, 1H), 7.51 (s, 1H), 7.36 (m, 3H), 7.16 (M + H)⁺[1-(tetrahydro- (m, 2H), 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.69 (t,2H-pyran-4- J = 6.0 Hz, 1H), 4.33 (d, J = 5.9 Hz, 2H), 3.90-ylacetyl)pyrro- 3.72 (m, 3H), 3.67-3.40 (m, 2H), 3.27-3.08 lidin-3- (m,2H), 3.14 (m, 1H), 2.28-2.10 (m, 3H), yl]phenyl}urea 2.00-1.80 (m, 3H),1.59 (m, 2H), 1.17 (m, 2H) 392 1-(imidazo[1,2- - ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.65 (ESI(+)) a]pyridin-7- (d, J = 6.1 Hz, 1H), 8.48 (d,J = 6.9 Hz, 1H), m/e 463 ylmethyl)-3-{4- 7.88 (s, 1H), 7.51 (d, J = 1.2Hz, 1H), 736 (m, (M + H)⁺ [1-(morpholin-4- 3H), 7.16 (m, 2H), 6.83 (dd,J = 6.9, 1.7 Hz, ylacetyl)pyrro- 1H), 6.72 (td, J = 6.0, 2.3 Hz, 1H),4.33 (d, J = lidin-3- 5.9 Hz, 2H), 3.74 (m, 1H), 3.55 (m, 4H), 3.45-yl]phenyl}urea 3.20 (m, 2H), 3.17 (s, 2H), 3.13-3.03 (m, 2H), 2.44 (m,4H), 2.30-2.10 (m, 1H), 2.00-1.80 (m, 1H)

Example 393N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamideExample 393A methyl4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(methoxycarbonyl)benzoic acid for 4-nitrobenzoic acid.

Example 393B 4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoate for methyl4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 393CN-(imidazo[1,2-a]pyridin-6-ylmethyl)-N′-(3-methylbutyl)benzene-1,4-dicarboxamide

The title compound was prepared as described in Example 1A, substituting3-methylbutan-1-amine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.25-9.11 (m, 1H),8.57-8.37 (m, 2H), 8.04-7.81 (m, 5H), 7.51 (t, J=2.6 Hz, 1H), 7.41 (t,J=2.9 Hz, 1H), 6.87 (dd, J=7.0, 1.7 Hz, 1H), 4.58-4.38 (m, 2H),3.29-3.25 (m, 2H), 1.71-1.56 (m, 1H), 1.53-1.31 (m, 2H), 0.91 (d, J=6.5Hz, 6H); MS (ESI(+)) m/e 365 (M+H)⁺.

Example 394N-(imidazo[1,2-a]pyridin-7-ylmethyl)-N′-[(3S)-tetrahydrofuran-3-ylmethyl]benzene-1,4-dicarboxamide

The title compound was prepared as described in Example 1A, substituting(S)-(tetrahydrofuran-3-yl)methanamine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.21 (t, J=5.9 Hz,1H), 8.69 (t, J=5.7 Hz, 1H), 8.49 (dd, J=6.9, 0.9 Hz, 1H), 8.07-7.71 (m,5H), 7.52 (d, J=1.2 Hz, 1H), 7.41 (s, 1H), 6.87 (dd, J=7.0, 1.7 Hz, 1H),4.52 (d, J=5.9 Hz, 2H), 3.80-3.56 (m, 4H), 3.48 (dd, J=8.5, 5.2 Hz, 1H),2.02-1.87 (m, 1H), 1.68-1.53 (m, 1H), 1.32-1.00 (m, 2H); MS (ESI(+)) m/e379 (M+H)⁺.

Example 3964-{[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]amino}-N-(tetrahydro-2H-pyran-2-ylmethyl)benzamide

A solution of4-(3-imidazo[1,2-a]pyridin-6-ylureido)-N-((tetrahydro-2H-pyran-2-yl)methyl)benzamide(0.016 g, 0.041 mmol) in chloroform (0.813 ml) was treated withN-chlorosuccinimide (5.70 mg, 0.043 mmol) and the reaction mixture wasstirred at room temperature for 16 hours. The reaction mixture wasconcentrated under a stream of nitrogen and purified using normal phasechromatography to give the title compound. ¹H NMR (400 MHz, DMSO-d₆) δppm 9.11 (s, 1H), 9.02 (s, 1H), 8.89-8.85 (m, 1H), 8.35 (t, J=5.8 Hz,1H), 7.85-7.79 (m, 2H), 7.69-7.60 (m, 2H), 7.58-7.52 (m, 2H), 7.19 (dd,J=9.5, 2.0 Hz, 1H), 3.91-3.83 (m, 1H), 3.46-3.19 (m, 4H), 1.80-1.73 (m,1H), 1.66-1.57 (m, 1H), 1.49-1.36 (m, 3H), 1.26-1.09 (m, 1H); MS(ESI(+)) m/e 428 (M+H)⁺.

Example 398N-[(3-chloroimidazo[1,2-a]pyridin-6-yl)methyl]-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamide

The title compound was prepared as described in Example 396,substitutingN-[(3-imidazo[1,2-a]pyridin-6-yl)methyl]-4-[(tetrahydrofuran-3-ylacetyl)amino]benzamidefor4-(3-imidazo[1,2-a]pyridin-6-ylureido)-N-((tetrahydro-2H-pyran-2-yl)methyl)benzamide.¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.15 (s, 1H), 8.95 (t, J=5.8 Hz, 1H),8.30-8.25 (m, 1H), 7.87-7.80 (m, 2H), 7.71-7.59 (m, 4H), 7.35 (dd,J=9.3, 1.7 Hz, 1H), 4.54 (d, J=5.8 Hz, 2H), 3.86-3.58 (m, 3H), 3.38-3.30(m, 1H), 2.62-2.52 (m, 1H), 2.47-2.39 (m, 2H), 2.10-1.95 (m, 1H),1.62-1.46 (m, 1H); MS (ESI(+)) m/e 413 (M+H)⁺.

Example 3995-(4-hydroxytetrahydro-2H-pyran-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 399A 5-(4-hydroxytetrahydro-2H-pyran-4-yl)thiophene-2-carboxylicacid

The title compound was prepared as described in Example 324A,substituting dihydro-2H-pyran-4(3H)-one forN-(oxetan-3-ylidene)propane-2-sulfinamide.

Example 399B5-(4-hydroxytetrahydro-2H-pyran-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(4-hydroxytetrahydro-2H-pyran-4-yl)thiophene-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.99 (t, J=5.9 Hz,1H), 8.48 (d, J=7.1 Hz, 1H), 7.88 (s, 1H), 7.66 (d, J=3.7 Hz, 1H), 7.52(s, 1H), 7.37 (s, 1H), 7.02 (d, J=3.7 Hz, 1H), 6.83 (dd, J=7.0, 1.5 Hz,1H), 5.67 (s, 1H), 4.46 (d, J=6.1 Hz, 2H), 3.63-3.77 (m, 4H), 1.89-2.04(m, 2H), 1.69 (d, J=11.9 Hz, 2H); MS (ESI(+)) m/e 358 (M+H)⁺.

Example 4005-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 400A5-(1-(tert-butoxycarbonyl)-3-hydroxyazetidin-3-yl)thiophene-2-carboxylicacid

The title compound was prepared as described in Example 324A,substituting tert-butyl 3-oxoazetidine-1-carboxylate forN-(oxetan-3-ylidene)propane-2-sulfinamide.

Example 400B tert-butyl3-hydroxy-3-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)azetidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(1-(tert-butoxycarbonyl)-3-hydroxyazetidin-3-yl)thiophene-2-carboxylicacid for 4-nitrobenzoic acid.

Example 400C5-(3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-hydroxy-3-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)azetidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 400D5-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.06 (t, J=6.0 Hz, 1H), 8.49 (d, J=7.1Hz, 1H), 7.89 (s, 1H), 7.72 (d, J=3.6 Hz, 1H), 7.52 (s, 1H), 7.38 (s,1H), 7.18 (d, J=3.6 Hz, 1H), 6.90 (s, 1H), 6.83 (dd, J=6.9, 1.4 Hz, 1H),4.47 (d, J=6.0 Hz, 2H), 4.41 (d, J=9.1 Hz, 1H), 4.32 (d, J=9.1 Hz, 1H),4.05 (dd, J=17.5, 9.9 Hz, 2H), 2.46-2.57 (m, 1H), 1.00 (d, J=7.1 Hz,6H); MS (ESI(+)) m/e 399 (M+H)⁺.

Example 4015-(1-benzoyl-3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.05 (t, J=5.8 Hz, 1H), 8.48 (d, J=6.1 Hz,1H), 7.88 (s, 1H), 7.73 (d, J=3.7 Hz, 1H), 7.66-7.71 (m, 2H), 7.43-7.54(m, 4H), 7.38 (d, J=1.0 Hz, 1H), 7.26 (d, J=3.7 Hz, 1H), 6.93 (s, 1H),6.83 (dd, J=7.1, 1.7 Hz, 1H), 4.46 (d, J=6.1 Hz, 2H), 4.23-4.63 (br. m,4H); MS (ESI(+)) m/e 433 (M+H)⁺.

Example 402 tert-butyl3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}azetidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)azetidin-3-yl)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.09 (t, J=5.9 Hz, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.91 (m, 3H), 7.52 (d, J=1.2 Hz, 1H), 7.45 (m, 2H),7.38 (s, 1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 4.51 (d, J=5.9 Hz, 2H), 4.26(m, 2H), 3.87 (m, 3H), 1.41 (s, 9H); (ESI(+)) m/e 407 (M+H)⁺.

Example 403 tert-butyl4-hydroxy-4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylateExample 403A5-(1-(tert-butoxycarbonyl)-4-hydroxypiperidin-4-yl)thiophene-2-carboxylicacid

The title compound was prepared as described in Example 324A,substituting tert-butyl 3-oxopiperidine-1-carboxylate forN-(oxetan-3-ylidene)propane-2-sulfinamide.

Example 403B tert-butyl4-hydroxy-4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(1-(tert-butoxycarbonyl)-4-hydroxypiperidin-4-yl)thiophene-2-carboxylicacid for 4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.98 (t,J=5.9 Hz, 1H), 8.48 (d, J=7.1 Hz, 1H), 7.88 (s, 1H), 7.65 (d, J=4.1 Hz,1H), 7.51 (d, J=1.0 Hz, 1H), 7.37 (s, 1H), 7.01 (d, J=3.7 Hz, 1H), 6.83(dd, J=7.0, 1.5 Hz, 1H), 5.72 (s, 1H), 4.46 (d, J=5.8 Hz, 2H), 3.75-3.86(m, 2H), 1.71-1.86 (m, 2H), 1.41 (s, 9H), 1.21-1.30 (m, 2H), 0.94 (d,J=5.8 Hz, 2H); MS (ESI(+)) m/e 457 (M+H)⁺.

Example 4041-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[5-(piperidin-1-ylcarbonyl)-1,3-thiazol-2-yl]ureaExample 404A ethyl2-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)thiazole-5-carboxylate

The title compound was prepared as described in Example 1C, substitutingethyl 2-aminothiazole-5-carboxylate for 4-amino-N-isopentylbenzamide andimidazo[1,2-a]pyridin-7-ylmethanamine for imidazo[1,2-a]pyridin-6-amine.

Example 404B2-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)thiazole-5-carboxylic acid

The title compound was prepared as described in Example 4B, substitutingethyl2-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)thiazole-5-carboxylate formethyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 404C1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[5-(piperidin-1-ylcarbonyl)-1,3-thiazol-2-yl]urea

The title compound was prepared as described in Example 1A, substitutingpiperidine for 3-methylbutan-1-amine and2-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)thiazole-5-carboxylic acidfor 4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.91 (s, 1H),8.49 (d, J=7.1 Hz, 1H), 7.89 (s, 1H), 7.62 (s, 1H), 7.52 (d, J=0.8 Hz,1H), 7.39 (s, 1H), 7.11-7.18 (m, 1H), 6.83 (dd, J=6.9, 1.4 Hz, 1H), 4.39(d, J=6.0 Hz, 2H), 3.54-3.61 (m, 4H), 1.47-1.67 (m, 6H); MS (ESI(+)) m/e385 (M+H)⁺.

Example 4055-{3-hydroxy-1-[(2S)-2-methylbutanoyl]azetidin-3-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) ppm 9.06 (t, J=5.9 Hz,1H), 8.48 (d, J=7.1 Hz, 1H), 7.88 (s, 1H), 7.72 (d, J=4.1 Hz, 1H), 7.52(d, J=1.4 Hz, 1H), 7.38 (s, 1H), 7.16 (dd, J=7.0, 3.9 Hz, 1H), 6.89 (s,1H), 6.83 (dd, J=7.0, 1.5 Hz, 1H), 4.46 (d, J=6.1 Hz, 2H), 4.35-4.42 (m,1H), 4.32 (d, J=8.8 Hz, 1H), 4.09 (dd, J=10.5, 4.4 Hz, 1H), 4.03 (d,J=10.2 Hz, 1H), 2.25-2.38 (m, 1H), 1.49 (s, 1H), 1.23-1.38 (m, 1H), 0.99(d, J=6.8 Hz, 3H), 0.80-0.88 (m, 3H); MS (ESI(+)) m/e 413 (M+H)⁺.

Example 4065-[3-hydroxy-1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-hydroxyazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 2-(tetrahydro-2H-pyran-4-yl)acetic acidfor 4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.07 (t, J=6.0Hz, 1H), 8.49 (d, J=7.0 Hz, 1H), 7.89 (s, 1H), 7.72 (d, J=4.0 Hz, 1H),7.52 (d, J=1.2 Hz, 1H), 7.38 (s, 1H), 7.18 (d, J=4.0 Hz, 1H), 6.89 (s,1H), 6.83 (dd, J=7.0, 1.5 Hz, 1H), 4.47 (d, J=5.8 Hz, 2H), 4.37 (d,J=9.2 Hz, 1H), 4.26-4.40 (m, 2H), 4.05-4.11 (m, 1H), 4.00-4.10 (m, 2H),3.78-3.84 (m, 2H), 2.04-2.07 (m, 2H), 1.85-1.97 (m, 1H), 1.53-1.62 (m,2H), 1.15-1.28 (m, 2H); MS (ESI(+)) m/e 455 (M+H)⁺.

Example 4072-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}-N-(3-methylbutyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substituting3-methylbutan-1-amine for 3-methylbutan-1-amine and2-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)thiazole-5-carboxylic acidfor 4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.49 (d, J=7.8Hz, 1H), 8.21 (t, J=5.9 Hz, 1H), 7.88-7.89 (m, J=1.4 Hz, 1H), 7.87 (s,1H), 7.52 (d, J=1.4 Hz, 1H), 7.39 (s, 1H), 7.18 (t, J=5.8 Hz, 1H), 6.83(dd, J=6.8, 1.7 Hz, 1H), 4.38 (d, J=6.1 Hz, 2H), 3.16-3.25 (m, 2H),1.52-1.67 (m, 1H), 1.38 (q, J=6.9 Hz, 2H), 0.83-0.91 (m, 7H); MS(ESI(+)) m/e 387 (M+H)⁺.

Example 408N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(3-{[(2S)-2-methylbutanoyl]amino}oxetan-3-yl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(3-aminooxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.11 (s, 1H), 9.05(t, J=5.9 Hz, 1H), 8.48 (d, J=7.8 Hz, 1H), 7.88 (s, 1H), 7.71 (d, J=3.7Hz, 1H), 7.52 (s, 1H), 7.38 (s, 1H), 7.22 (d, J=3.7 Hz, 1H), 6.83 (dd,J=7.1, 1.7 Hz, 1H), 4.77-4.83 (m, 2H), 4.72 (dd, J=6.4, 4.4 Hz, 2H),4.46 (d, J=5.8 Hz, 2H), 2.19-2.29 (m, 1H), 1.46-1.66 (m, 1H), 1.26-1.43(m, 1H), 1.03 (d, J=6.8 Hz, 3H), 0.85 (t, J=7.3 Hz, 3H); MS (ESI(+)) m/e413 (M+H)⁺.

Example 409N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1-[1-(3-methylbutanoyl)piperidin-4-yl]-1H-pyrazole-3-carboxamideExample 409A 1-(4-hydroxypiperidin-1-yl)-3-methylbutan-1-one

The title compound was prepared as described in Example 52A,substituting 3-methylbutanoyl chloride for 2-cyclopentylacetyl chlorideand piperidin-4-ol for methyl 4-aminobenzoate.

Example 409B ethyl1-(1-(3-methylbutanoyl)piperidin-4-yl)-1H-pyrazole-3-carboxylate

A solution of 1-(hydroxypiperidin-1-yl)-3-methylbutan-1-one (793 mg,4.28 mmol), ethyl 1H-pyrazole-4-carboxylate (500 mg, 3.57 mmol) andcyanomethylenetributylphosphorane (1.03 g, 4.28 mmol) in toluene (20 ml)was stirred overnight at 85° C. The solvent was removed and the crudemixture was purified by normal phase chromatography to give the titlecompound.

Example 409C1-(1-(3-methylbutanoyl)piperidin-4-yl)-1H-pyrazole-3-carboxylic acid

The title compound was prepared as described in Example 4B, substitutingethyl 1-(1-(3-methylbutanoyl)piperidin-4-yl)-1H-pyrazole-3-carboxylatefor methyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 409DN-(imidazo[1,2-a]pyridin-7-ylmethyl)-1-[1-(3-methylbutanoyl)piperidin-4-yl]-1H-pyrazole-3-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and1-(1-(3-methylbutanoyl)piperidin-4-yl)-1H-pyrazole-3-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.10 (t, J=6.0 Hz,1H), 8.50 (dd, J=7.0, 0.9 Hz, 1H), 7.93-7.86 (m, 1H), 7.57-7.47 (m, 2H),7.41 (s, 1H), 6.92 (d, J=2.0 Hz, 1H), 6.85 (dd, J=7.0, 1.7 Hz, 1H),5.45-5.28 (m, 1H), 4.57-4.43 (m, 3H), 3.99 (d, J=14.0 Hz, 1H), 3.20-3.03(m, 1H), 2.70-2.53 (m, 1H), 2.32-2.11 (m, 3H), 2.09-1.68 (m, 4H), 0.91(d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 408 (M+H).

Example 4241-{4-[(1-acetylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureaExample 424A tert-butyl3-(4-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)phenoxy)azetidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 3-(4-aminophenoxy)azetidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine.

Example 424B1-(4-(azetidin-3-yloxy)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl3-(4-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)phenoxy)azetidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 424C1-{4-[(1-acetylazetidin-3-yl)oxy]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(4-(azetidin-3-yloxy)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 3-methylbutan-1-amine and acetic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 8.50 (m, 2H), 7.88 (s, 1H), 7.51 (d, J=1.2Hz, 1H), 7.37 (m, 1H), 7.33 (m, 2H), 6.83 (dd, J=6.9, 1.6 Hz, 1H), 6.74(m, 2H), 6.63 (t, J=6.0 Hz, 1H), 4.93 (m, 1H), 4.51 (m, 1H), 4.32 (d,J=6.0 Hz, 2H), 4.24 (m, 1H), 4.04 (dd, J=9.6, 4.1 Hz, 1H), 3.72 (dd,J=10.5, 4.0 Hz, 1H), 1.78 (s, 3H); (ESI(+)) m/e 380 (M+H)⁺.

TABLE 20 The following Examples were prepared essentially as describedin Example 424, substituting the appropriate carboxylic acid in Example424C. Ex Name ¹H NMR MS 425 1-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δppm 8.49 (m, (ESI(+)) a]pyridin-7- 2H), 7.88 (s, 1H), 7.51 (d, J = 1.2Hz, 1H), 7.37 m/e 408 ylmethyl)-3-(4- (m, 1H), 7.33 (m, 2H), 6.83 (dd, J= 6.9, 1.7 Hz, (M + H)⁺ {[1-(2- 1H), 6.75 (m, 2H), 6.63 (t, J = 6.0 Hz,1H), 4.95 methylpropanoyl)azetidin- (m, 1H), 4.57 (dd, J = 9.4, 6.4 Hz,1H), 4.32 (d, J = 3- 6.0 Hz, 2H), 4.25 (dd, J = 10.5, 6.5 Hz, 1H),yl]oxy}phenyl)urea 4.08 (dd, J = 9.4, 3.9 Hz, 1H), 3.73 (dd, J = 10.5,4.0 Hz, 1H), 2.47 (m, 1H), 0.97 (m, 6H) 426 1-(imidazo[1,2- ¹H NMR (400MHz, DMSO-d₆) δ ppm 8.49 (m, (ESI(+)) a]pyridin-7- 2H), 7.88 (d, J = 1.1Hz, 1H), 7.51 (d, J = 1.2 Hz, m/e 422 ylmethyl)-3-[4- 1H), 7.37 (m, 1H),7.33 (m, 2H), 6.83 (dd, J = 6.9, (M + H)⁺ ({1-[(2S)-2- 1.6 Hz, 1H), 6.75(m, 2H), 6.64 (t, J = 6.0 Hz, methylbutanoyl]azetidin- 1H), 4.95 (m,1H), 4.56 (dd, J = 9.4, 6.5 Hz, 1H), 3- 4.32 (d, J = 6.0 Hz, 2H), 4.26(m, 1H), 4.08 (m, yl}oxy)phenyl]urea 1H), 3.74 (m, 1H), 2.28 (m, 1H),1.47 (m, 1H), 1.28 (m, 1H), 0.95 (m, 3H), 0.81 (m, 3H) 427 1-(4-{[1- ¹HNMR (400 MHz, DMSO-d₆) δ ppm 8.49 (m, (ESI(+)) (cyclopro- 2H), 7.90 (s,1H), 7.54 (d, J = 1.2 Hz, 1H), 7.39 m/e 420 pylacetyl)azetidin-3- (s,1H), 7.33 (m, 2H), 6.86 (dd, J = 7.0, 1.6 Hz, (M + H)⁺ yl]oxy}phenyl)-1H), 6.74 (m, 2H), 6.64 (t, J = 6.0 Hz, 1H), 4.94 3-(imidazo[1,2- (m,1H), 4.50 (dd, J = 9.6, 6.6 Hz, 1H), 4.33 (d, J = a]pyridin-7- 6.0 Hz,2H), 4.26 (dd, J = 10.5, 6.5 Hz, 1H), ylmethyl)urea 4.03 (dd, J = 9.4,3.9 Hz, 1H), 3.74 (dd, J = 10.5, 3.9 Hz, 1H), 2.02 (d, J = 6.8 Hz, 2H),0.92 (m, 1H), 0.43 (m, 2H), 0.10 (m, 2H) 428 1-{4-[(1- ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.49 (m, (ESI(+)) benzoylazetidin- 2H), 7.88 (s, 1H),7.65 (m, 2H), 7.52 (m, 2H), m/e 442 3- 7.45 (m, 2H), 7.37 (m, 1H), 7.33(m, 2H), 6.83 (M + H)⁺ yl)oxy]phenyl}- (dd, J = 6.9, 1.6 Hz, 1H), 6.75(m, 2H), 6.63 (t, J = 3-(imidazo[1,2- 6.0 Hz, 1H), 5.00 (m, 1H), 4.67(m, 1H), 4.51 a]pyridin-7- (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), 4.26 (m,1H), ylmethyl)urea 3.97 (m, 1H) 429 1-(imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.49 (m, (ESI(+)) a]pyridin-7- 2H), 7.88 (s, 1H), 7.51(d, J = 1.2 Hz, 1H), 7.37 m/e 438 ylmethyl)-3-[4- (s, 1H), 7.33 (m, 2H),6.83 (dd, J = 6.9, 1.6 Hz, (M + H)⁺ ({1-[(propan-2- 1H), 6.74 (m, 2H),6.64 (t, J = 6.0 Hz, 1H), 4.96 yloxy)acetyl]azetidin- (m, 1H), 4.60 (dd,J = 10.1, 6.4 Hz, 1H), 4.30 (m, 3- 3H), 4.11 (dd, J = 10.1, 3.9 Hz, 1H),3.94 (s, 2H), yl}oxy)phenyl]urea 3.77 (dd, J = 10.7, 3.8 Hz, 1H), 3.58(m, 1H), 1.09 (d, J = 6.1 Hz, 6H) 430 1-(4-{[1-(2- ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.48 (m, (ESI(+)) hydroxy-2- 2H), 7.88 (s, 1H), 7.51 (s,1H), 7.38 (s, 1H), 7.33 m/e 424 methylpropanoyl)azetidin- (m, 2H), 6.83(dd, J = 6.9, 1.6 Hz, 1H), 6.74 (m, (M + H)⁺ 3- 2H), 6.63 (t, J = 6.0Hz, 1H), 5.13 (s, 1H), 4.91 yl]oxy}phenyl)- (m, 1H), 4.78 (m, 1H), 4.32(d, J = 6.0 Hz, 3H), 3-(imidazo[1,2- 4.26 (m, 1H), 3.73 (m, 1H), 1.25(s, 6H) a]pyridin-7- ylmethyl)urea 431 1-(imidazo[1,2- ¹H NMR (400 MHz,DMSO-d₆) δ ppm 8.49 (m, (ESI(+)) a]pyridin-7- 2H), 7.88 (s, 1H), 7.51(d, J = 1.2 Hz, 1H), 7.37 m/e 436 ylmethyl)-3-[4- (s, 1H), 7.33 (m, 2H),6.83 (dd, J = 6.9, 1.6 Hz, (M + H)⁺ ({1-[(2R)- 1H), 6.74 (m, 2H), 6.63(t, J = 6.0 Hz, 1H), 4.95 tetrahydrofuran- (m, 1H), 4.66 (m, 1H), 4.31(m, 4H), 4.13 (m, 2- 1H), 3.75 (m, 3H), 2.03 (m, 1H), 1.93 (m, 1H),ylcarbonyl]azetidin- 1.81 (m, 2H) 3- yl}oxy)phenyl]urea 4321-(imidazo[1,2- - ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.49 (m, (ESI(+))a]pyridin-7- 2H), 7.88 (s, 1H), 7.51 (d, J = 1.2 Hz, 1H), 7.37 m/e 436ylmethyl)-3-[4- (s, 1H), 7.33 (m, 2H), 6.83 (dd, J = 6.9, 1.6 Hz, (M +H)⁺ ({1-[(2S)- 1H), 6.74 (m, 2H), 6.64 (t, J = 6.0 Hz, 1H), 4.95tetrahydrofuran- (m, 1H), 4.66 (m, 1H), 4.3123 (m, 4H), 4.13 (m, 2- 1H),3.75 (m, 3H), 2.03 (m, 1H), 1.93 (m, 1H), ylcarbonyl]azetidin- 1.81 (m,2H) 3- yl}oxy)phenyl]urea 433 1-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆)δ ppm 8.48 (m, (ESI(+)) a]pyridin-7- 2H), 7.88 (d, J = 1.1 Hz, 1H), 7.51(d, J = 1.2 Hz, m/e 450 ylmethyl)-3-(4- 1H), 7.37 (s, 1H), 7.33 (m, 2H),6.83 (dd, J = 6.9, (M + H)⁺ {[1-(tetrahydro- 1.7 Hz, 1H), 6.74 (m, 2H),6.64 (t, J = 6.0 Hz, 2H-pyran-4- 1H), 4.95 (m, 1H), 4.60 (dd, J = 9.4,6.5 Hz, 1H), ylcarbonyl)azetidin- 4.32 (d, J = 6.0 Hz, 3H), 4.26 (m,1H), 4.11 (dd, J = 3- 9.5, 3.8 Hz, 1H), 3.84 (m, 2H), 3.74 (dd, J =yl]oxy}phenyl)urea 10.6, 3.9 Hz, 1H), 3.36-3.26 (m, 2H), 1.57 (m, 4H)434 1-(4-{[1-(1,4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.48 (d, (ESI(+))dioxan-2- 2H), 7.88 (s, 1H), 7.51 (s, 1H), 7.37 (s, 1H), 7.33 m/e 452ylcarbonyl)azetidin- (m, 2H), 6.83 (dd, J = 6.9, 1.6 Hz, 1H), 6.74 (m,(M + H)⁺ 3- 2H), 6.64 (t, J = 6.0 Hz, 1H), 4.96 (m, 1H), 4.69yl]oxy}phenyl)- (m, 1H), 4.30 (m, 3H), 4.18 (m, 2H), 3.76 (m,3-(imidazo[1,2- 3H), 3.65-3.45 (m, 4H) a]pyridin-7- ylmethyl)urea 4351-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.51 (s, (ESI(+))a]pyridin-7- 1H), 8.48 (dd, J = 6.9, 0.9 Hz, 1H), 7.88 (d, J = m/e 464ylmethyl)-3-(4- 1.1 Hz, 1H), 7.51 (d, J = 1.2 Hz, 1H), 7.37 (s, (M + H)⁺{[1-(tetrahydro- 1H), 7.33 (m, 2H), 6.83 (dd, J = 6.9, 1.7 Hz, 1H),2H-pyran-4- 6.74 (m, 2H), 6.64 (t, J = 6.0 Hz, 1H), 4.94 (m,ylacetyl)azetidin- 1H), 4.52 (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), 4.25 3-(m, 1H), 4.04 (dd, J = 9.5, 3.9 Hz, 1H), 3.76 (m, yl]oxy}phenyl)urea3H), 3.27 (m, 2H), 2.02 (d, J = 1.9 Hz, 2H), 1.87 (m, 1H), 1.54 (m, 2H),1.19 (m, 2H)

Example 436 tert-butyl(3R)-3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 321A-C,substituting (S)-tert-butyl 3-hydroxypyrrolidine-1-carboxylate for(R)-tert-butyl 3-hydroxypyrrolidine-1-carboxylate in Example 321A. ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.41-8.35 (m, 1H), 7.91-7.83 (m, 2H),7.81-7.76 (m, 1H), 7.52 (d, J=1.4 Hz, 1H), 7.47-7.43 (m, 1H), 7.06-6.98(m, 2H), 6.93 (dd, J=7.1, 1.5 Hz, 1H), 5.12-5.05 (m, 1H), 4.62 (bs, 2H),3.68-3.39 (m, 4H), 2.25-2.13 (m, 2H), 1.49-1.43 (m, 9H).; MS (ESI(+))m/e 437 (M+H)⁺.

Example 4381-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureaExample 438A1-(2-fluoro-4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)-3,6-dihydropyridine-1(2H)-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 438B1-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(2-fluoro-4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.77-8.70 (m, 1H), 8.19-8.15 (m, 1H),8.00-7.96 (m, 1H), 7.95-7.88 (m, 1H), 7.80 (s, 1H), 7.53-7.41 (m, 6H),7.30-7.15 (m, 2H), 6.26-5.95 (m, 1H), 4.61 (bs, 2H), 4.41-4.31 (m, 1H),4.17-4.08 (m, 1H), 4.02-3.93 (m, 1H), 3.69-3.59 (m, 1H), 2.67-2.52 (m,2H); MS (ESI(+)) m/e 470 (M+H)⁺.

Example 4391-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(2-fluoro-4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 3-methylbutan-1-amine and 2-(tetrahydro-2H-pyran-4-yl)acetic acidfor 4-nitrobenzoic acid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.74 (dd,J=7.0, 0.9 Hz, 1H), 8.18-8.15 (m, 1H), 7.98 (d, J=2.2 Hz, 1H), 7.92 (t,J=8.5 Hz, 1H), 7.82-7.78 (m, 1H), 7.47 (dd, J=7.0, 1.6 Hz, 1H),7.28-7.15 (m, 2H), 6.16-6.10 (m, 1H), 4.61 (bs, 2H), 4.25-4.16 (m, 2H),3.96-3.87 (m, 2H), 3.83-3.72 (m, 2H), 3.48-3.37 (m, 2H), 2.61-2.54 (m,1H), 2.53-2.46 (m, 1H), 2.45-2.34 (m, 2H), 2.11-1.97 (m, 1H), 1.73-1.62(m, 2H), 1.42-1.27 (m, 2H); MS (ESI(+)) m/e 492 (M+H)⁺.

Example 4421-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)ureaExample 442A1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(piperidin-4-yloxy)phenyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenoxy)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 442B1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-{[1-(2-methylpropanoyl)piperidin-4-yl]oxy}phenyl)urea

The title compound was prepared as described in Example 1A, substituting1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(piperidin-4-yloxy)phenyl)ureafor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.48 (m, 2H), 7.88 (s, 1H), 7.51 (s,1H), 7.37 (s, 1H), 7.31 (m, 2H), 6.87 (m, 2H), 6.83 (dd, J=7.0, 1.6 Hz,1H), 6.62 (t, J=6.0 Hz, 1H), 4.48 (m, 1H), 4.32 (d, J=6.0 Hz, 2H), 3.85(m, 1H), 3.74 (m, 1H), 3.35 (m, 1H), 3.22 (m, 1H), 2.88 (m, 1H), 1.88(m, 2H), 1.49 (m, 2H), 0.99 (d, J=6.7 Hz, 6H); (ESI(+)) m/e 436 (M+H).

TABLE 21 The following Examples were prepared essentially as describedin Example 442, substituting the appropriate carboxylic acid in Example442B. Ex Name ¹H NMR MS 443 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δppm 8.48 (ESI(+)) a]pyridin-7- (m, 2H), 7.88 (s, 1H), 7.51 (s, 1H), 7.37(s, m/e 450 ylmethyl)-3-[4-({1- 1H), 7.31 (m, 2H), 6.87 (m, 2H), 6.83(dd, J = (M + H)⁺ [(2S)-2- 7.0, 1.6 Hz, 1H), 6.65 (t, J = 6.0 Hz, 1H),4.49 methylbutanoyl]piper- (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), 3.84 (m,idin-4- 2H), 3.26 (m, 2H), 2.72 (m, 1H), 1.90 (m, yl}oxy)phenyl]urea2H), 1.51 (m, 3H), 1.29 (m, 1H), 0.97 (d, J = 6.7 Hz, 3H), 0.81 (t, J =7.4 Hz, 3H) 444 1-(4-{[1- - ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.48(ESI(+)) (cyclopropylacetyl) (m, 2H), 7.88 (s, 1H), 7.51 (s, 1H), 7.37(s, m/e 448 piperidin-4- 1H), 7.31 (m, 2H), 6.87 (m, 2H), 6.83 (dd, J =(M + H)⁺ yl]oxy}phenyl)-3- 7.0, 1.6 Hz, 1H), 6.62 (t, J = 6.0 Hz, 1H),4.47 (imidazo[1,2- (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), 3.85 (m,a]pyridin-7- 1H), 3.66 (m, 1H), 3.30 (m, 1H), 3.22 (m, ylmethyl)urea1H), 2.26 (d, J = 6.8 Hz, 2H), 1.91 (m, 2H), 1.50 (m, 2H), 0.95 (m, 1H),0.44 (m, 2H), 0.11 (m, 2H) 445 1-{4-[(1- ¹H NMR (500 MHz, DMSO-d₆) δ ppm8.48 (ESI(+)) benzoylpiperidin-4- (m, 2H), 7.88 (s, 1H), 7.51 (s, 1H),7.44 (m, m/e 470 yl)oxy]phenyl}-3- 3H), 7.40 (m, 2H), 7.37 (m, 1H), 7.31(m, (M + H)⁺ (imidazo[1,2- 2H), 6.87 (m, 2H), 6.83 (dd, J = 7.0, 1.6 Hz,a]pyridin-7- 1H), 6.63 (t, J = 6.0 Hz, 1H), 4.52 (m, 1H), ylmethyl)urea4.31 (d, J = 6.0 Hz, 2H), 3.96 (m, 1H), 3.52 (m, 1H), 3.45-3.20 (m, 2H),1.91 (m, 2H), 1.59 (m, 2H) 446 1-(imidazo[1,2- ¹H NMR (400 MHz, DMSO-d₆)δ ppm 8.48 (ESI(+)) a]pyridin-7- (m, 2H), 7.88 (m, 1H), 7.51 (d, J = 1.2Hz, m/e 466 ylmethyl)-3-[4-({1- 1H), 7.37 (m, 1H), 7.31 (m, 2H), 6.87(m, (M + H)⁺ [(propan-2- 2H), 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.64 (m,yloxy)acetyl]piper- 1H), 4.49 (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), idin-4-4.08 (s, 2H), 3.82 (m, 1H), 3.67 (m, 1H), yl}oxy)phenyl]urea 3.59(m,1H), 3.40-3.15 (m, 2H), 1.90 (m, 2H), 1.52 (m, 2H), 1.10 (d, J = 6.1 Hz,6H) 447 1-(4-{[1-(2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.48 (ESI(+))hydroxy-2- (m, 2H), 7.88 (s, 1H), 7.52 (d, J = 1.2 Hz, m/e 452methylpropanoyl)piper- 1H), 7.38 (s, 1H), 7.30 (m, 2H), 6.87 (m, 2H),(M + H)⁺ idin-4- 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.62 (t, J = 6.0yl]oxy}phenyl)-3- Hz, 1H), 5.39 (s, 1H), 4.48 (m, 1H), 4.32 (d, J =(imidazo[1,2- 6.0 Hz, 2H), 4.10-3.40 (m, 2H), 3.40- a]pyridin-7- 3.15(m, 2H), 1.90 (m, 2H), 1.54 (m, 2H), ylmethyl)urea 1.31 (s, 6H) 4481-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.49 (ESI(+))a]pyridin-7- (m, 2H), 7.90 (s, 1H), 7.54 (d, J = 1.2 Hz, m/e 464ylmethyl)-3-[4-({1- 1H), 7.39 (s, 1H), 7.31 (m, 2H), 6.86 (m, 3H), (M +H)⁺ [(2R)- 6.62 (t, J = 6.0 Hz, 1H), 4.67 (m, 1H), 4.48tetrahydrofuran-2- (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), 3.78 (m,ylcarbonyl]piper- 4H), 3.45-3.15 (m, 2H), 2.10-1.75 (m, 6H), idin-4-1.53 (m, 2H) yl}oxy)phenyl]urea 449 1-(imidazo[1,2- ¹H NMR (500 MHz,DMSO-d₆) δ ppm 8.48 (ESI(+)) a]pyridin-7- (m, 2H), 7.89 (s, 1H), 7.52(d, J = 1.2 Hz, m/e 464 ylmethyl)-3-[4-({1- 1H), 7.38 (s, 1H), 7.31 (m,2H), 6.87 (m, 2H), (M + H)⁺ [(2S)- 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.62(t, J = 6.0 tetrahydrofuran-2- Hz, 1H), 4.67 (m, 1H), 4.48 (m, 1H), 4.32(d, ylcarbonyl]piper- J = 6.0 Hz, 2H), 3.78 (m, 4H), 3.45-3.16 (m,idin-4- 2H), 2.09-1.92 (m, 2H), 2.09-1.92 (m, 4H), yl}oxy)phenyl]urea1.53 (m, 2H) 450 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.48(ESI(+)) a]pyridin-7- (m, 2H), 7.88 (s, 1H), 7.51 (d, J = 1.2 Hz, m/e478 ylmethyl)-3-(4-{[1- 1H), 7.38 (s, 1H), 7.31 (m, 2H), 6.87 (m, 2H),(M + H)⁺ (tetrahydro-2H- 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.62 (t, J =6.0 pyran-4- Hz, 1H), 4.48 (m, 1H), 4.32 (d, J = 6.0 Hz,ylcarbonyl)piper- 2H), 3.88-3.71 (m, 4H), 3.38 (m, 2H), 3.34- idin-4-3.16 (m, 1H), 3.22 (m, 1H), 2.89 (m, 1H), yl]oxy}phenyl)urea 1.91 (m,2H), 1.67-1.40 (m, 6H) 451 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δppm 8.48 (ESI(+)) a]pyridin-7- (m, 2H), 7.88 (s, 1H), 7.52 (bs, 1H),7.38 (bs, m/e 492 ylmethyl)-3-(4-{[1- 1H), 7.31 (m, 2H), 6.87 (m, 2H),6.83 (dd, J = (M + H)⁺ (tetrahydro-2H- 7.0, 1.5 Hz, 1H), 6.62 (t, J =6.0 Hz, 1H), 4.47 pyran-4- (m, 1H), 4.32 (d, J = 6.0 Hz, 2H), 3.89-3.75ylacetyl)piper- (m, 3H), 3.70 (m, 1H), 3.40-3.17 (m, 4H), idin-4- 2.26(m, 2H), 1.89 (m, 3H), 1.60-1.40 (m, yl]oxy}phenyl)urea 4H), 1.19 (m,2H) 726 1-(4-{[1-(3- (ESI(+)) fluorobenzoyl)piper- m/e 488 idin-4- (M +H)⁺ yl]oxy}phenyl)-3- (imidazo[1,2- a]pyridin-7- ylmethyl)urea 7271-(4-{[1-(2,4- (ESI(+)) difluorobenzoyl)piper- m/e 506 idin-4- (M + H)⁺yl]oxy}phenyl)-3- (imidazo[1,2- a]pyridin-7- ylmethyl)urea 7281-(4-{[1-(2,5- (ESI(+)) difluorobenzoyl)piper- m/e 506 idin-4- (M + H)⁺yl]oxy}phenyl)-3- (imidazo[1,2- a]pyridin-7- ylmethyl)urea 7291-(4-{[1-(3,4- (ESI(+)) difluorobenzoyl)piper- m/e 506 idin-4- (M + H)⁺yl]oxy}phenyl)-3- (imidazo[1,2- a]pyridin-7- ylmethyl)urea 7301-(4-{[1-(3,5- difluorobenzoyl)piper- (ESI(+)) idin-4- m/e 506yl]oxy}phenyl)-3- (M + H)⁺ (imidazo[1,2- a]pyridin-7- ylmethyl)urea

Example 4521-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)azetidin-3-yl]phenyl}ureaExample 452A1-(4-(azetidin-3-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl3-(4-(3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureido)phenyl)azetidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 452B1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropanoyl)azetidin-3-yl]phenyl}urea

The title compound was prepared as described in Example 1A, substituting1-(4-(azetidin-3-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, DMSO-d₆) δ ppm 8.66 (s, 1H), 8.48 (d, J=7.0 Hz, 1H), 7.88(s, 1H), 7.51 (s, 1H), 7.39 (m, 3H), 7.22 (m, 2H), 6.83 (dd, J=7.0, 1.6Hz, 1H), 6.70 (t, J=6.0 Hz, 1H), 4.52 (m, 1H), 4.33 (d, J=6.0 Hz, 2H),4.20 (m, 1H), 4.08 (dd, J=8.5, 5.3 Hz, 1H), 3.76 (m, 2H), 2.49 (m, 1H),0.99 (d, J=6.8 Hz, 6H); (ESI(+)) m/e 392 (M+H)⁺.

TABLE 22 The following Examples were prepared essentially as describedin Example 452, substituting the appropriate carboxylic acid in Example452B. Ex Name ¹H NMR MS 453 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δppm 8.66 (s, (ESI(+)) a]pyridin-7- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88(s, 1H), 7.52 m/e 406 ylmethyl)-3-(4- (s, 1H), 7.40 (m, 3H), 7.22 (m,2H), 6.84 (dd, J = (M + H)⁺ {1-[(2S)-2- 7.0, 1.6 Hz, 1H), 6.70 (m, 1H),4.52 (m, 1H), methylbutan- 4.33 (d, J = 6.0 Hz, 2H), 4.21 (m, 1H), 4.06(m, oyl]azetidin-3- 1H), 3.76 (m, 2H), 2.27 (m, 1H), 1.50 (m, 1H),yl}phenyl)urea 1.30 (m, 1H), 0.98 (d, J = 6.8 Hz, 3H), 0.84 (t, J = 7.4Hz, 3H) 454 1-{4-[1- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.66 (s, (ESI(+))(cyclopropylace- 1H), 8.49 (d, J = 7.0 Hz, 1H), 7.89 (s, 1H), 7.53 m/e404 tyl)azetidin-3- (d, J = 1.2 Hz, 1H), 7.40 (m, 3H), 7.22 (m, 2H),(M + H)⁺ yl]phenyl}-3- 6.85 (dd, J = 7.0, 1.6 Hz, 1H), 6.70 (t, J = 6.0(imidazo[1,2- Hz, 1H), 4.45 (m, 1H), 4.33 (d, J = 6.0 Hz, 2H),a]pyridin-7- 4.20 (m, 1H), 4.04 (m, 1H), 3.75 (m, 2H), 2.02ylmethyl)urea (d, J = 6.8 Hz, 2H), 0.94 (m, 1H), 0.44 (m, 2H), 0.11 (m,2H) 455 1-[4-(1- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.68 (s, (ESI(+))benzoylazetidin- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 (s, 1H), 7.68 m/e426 3-yl)phenyl]-3- (m, 2H), 7.52 (m, 2H), 7.46 (m, 2H), 7.40 (m, (M +H)⁺ (imidazo[1,2- 3H), 7.26 (m, 2H), 6.83 (dd, J = 7.0, 1.6 Hz,a]pyridin-7- 1H), 6.72 (t, J = 6.0 Hz, 1H), 464 (m, 1H), 4.44ylmethyl)urea (m, 1H), 4.33 (d, J = 6.0 Hz, 2H), 4.27 (m, 1H), 3.98 (m,1H), 3.85 (m, 1H) 456 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm8.67 (s, (ESI(+)) a]pyridin-7- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 (s,1H), 7.51 m/e 422 ylmethyl)-3-(4- (d, J = 1.2 Hz, 1H), 7.40 (m, 3H),7.22 (m, 2H), (M + H)⁺ {1-[(propan-2- 6.83 (dd, J = 7.0, 1.6 Hz, 1H),6.71 (t, J = 6.0 yloxy)ace- Hz, 1H), 4.56 (m, 1H), 4.33 (d, J = 6.0 Hz,2H), tyl]azetidin-3- 4.24 (m, 1H), 4.13 (m, 1H), 3.95 (s, 2H), 3.79yl}phenyl)urea (m, 2H), 3.59 (m, 1H), 1.10 (d, J = 6.1 Hz, 6H) 4571-{4-[1-(2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.66 (s, (ESI(+)) hydroxy-2-1H), 8.50 (d, J = 7.0 Hz, 1H), 7.90 (s, 1H), 7.54 m/e 408methylpropanoyl) (d, J = 1.2 Hz, 1H), 7.40 (m, 3H), 7.21 (m, 2H), (M +H)⁺ azetidin-3- 6.86 (dd, J = 7.0, 1.6 Hz, 1H), 6.70 (t, J = 6.0yl]phenyl}-3- Hz, 1H), 5.09 (s, 1H), 4.75 (m, 1H), 4.32 (m,(imidazo[1,2- 3H), 4.22 (m, 1H), 3.74 (m, 2H), 1.27 (s, 6H) a]pyridin-7-ylmethyl)urea 458 1-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.73(s, (ESI(+)) a]pyridin-7- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 (s, 1H),7.51 m/e 420 ylmethyl)-3-(4- (s, 1H), 7.40 (m, 3H), 7.22 (m, 2H), 6.83(dd, J = (M + H)⁺ (1-[(2R)- 7.0, 1.6 Hz, 1H), 6.78 (t, J = 6.0 Hz, 1H),4.60 tetrahydrofuran-2- (m, 1H), 4.37 (m, 1H), 4.33 (d, J = 6.0 Hz, 2H),ylcarbon- 4.24 (m, 1H), 4.16 (m, 1H), 3.86-3.69 (m, yl]azetidin-3- 4H),2.04 (m, 1H), 1.96 (m, 1H), 1.82 (m, 2H) yl}phenyl)urea 4591-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.66 (s, (ESI(+))a]pyridin-7- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 (s, 1H), 7.51 m/e 420ylmethyl)-3-(4- (s, 1H), 7.40 (m, 3H), 7.22 (m, 2H), 6.83 (dd, J = (M +H)⁺ {1-[(2S)- 7.0, 1.6 Hz, 1H), 6.74-6.67 (m, 1H), 4.60tetrahydrofuran-2- (m, 1H), 4.37 (m, 1H), 4.33 (d, J = 6.0 Hz, 2H),ylcarbon- 4.23 (m, 1H), 4.15 (m, 1H), 3.85-3.69 (m, yl]azetidin-3- 4H),2.04 (m, 1H), 1.96 (m, 1H), 1.81 (m, 2H) yl}phenyl)urea 4601-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.67 (s, (ESI(+))a]pyridin-7- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 (s, 1H), 7.51 m/e 434ylmethyl)-3-{4- (d, J = 1.1 Hz, 1H), 7.40 (m, 3H), 7.22 (m, 2H), (M +H)⁺ [1-(tetrahydro- 6.83 (dd, J = 7.0, 1.6 Hz, 1H), 6.71 (t, J = 6.02H-pyran-4- Hz, 1H), 4.54 (m, 1H), 4.33 (d, J = 6.0 Hz, 2H), ylcarbon-4.21 (m, 1H), 4.13 (m, 1H), 3.85 (m, 2H), 3.77 yl)azetidin-3- (m, 2H),3.40-3.25 (m, 2H), 2.50 (m, 1H), yl]phenyl}urea 1.58 (m, 4H) 4611-(imidazo[1,2- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.70 (s, (ESI(+))a]pyridin-7- 1H), 8.48 (d, J = 7.0 Hz, 1H), 7.88 (s, 1H), 7.51 m/e 448ylmethyl)-3-{4- (s, 1H), 7.40 (m, 3H), 7.21 (m, 2H), 6.83 (dd, J = (M +H)⁺ [1-(tetrahydro- 7.0, 1.6 Hz, 1H), 6.75 (t, J = 6.0 Hz, 1H), 4.472H-pyran-4- (m, 1H), 4.33 (d, J = 6.0 Hz, 2H), 4.19 (m, 1H),ylacetyl)azetidin- 4.05 (m, 1H), 3.85-3.69 (m, 4H), 3.28 (m,3-yl]phenyl}urea 2H), 2.03 (d, J = 1.8 Hz, 2H), 1.90 (m, 1H), 1.57 (m,2H), 1.21 (m, 2H)

Example 4624-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamideExample 462A methyl 4-(2-cyclopentylacetamido)-2-fluorobenzoate

The title compound was prepared as described in Example 52A,substituting 2-cyclopentylacetyl chloride for 2-cyclopentylacetylchloride and methyl 4-amino-2-fluorobenzoate for methyl 4-aminobenzoate.

Example 462B 4-(2-cyclopentylacetamido)-2-fluorobenzoic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 4-(2-cyclopentylacetamido)-2-fluorobenzoate for methyl4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 462C4-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(2-cyclopentylacetamido)-2-fluorobenzoic acid for 4-nitrobenzoic acid.¹H NMR (501 MHz, DMSO-d₆) δ ppm 10.24 (s, 1H), 8.70-8.63 (m, 1H), 8.46(s, 1H), 7.95 (s, 1H), 7.74-7.62 (m, 2H), 7.58-7.50 (m, 2H), 7.32 (dd,J=8.5, 1.9 Hz, 1H), 7.24 (dd, J=9.2, 1.7 Hz, 1H), 4.45 (d, J=5.9 Hz,2H), 2.37-2.31 (m, 2H), 2.31-2.15 (m, 1H), 1.81-1.69 (m, 2H), 1.67-1.45(m, 4H), 1.25-1.12 (m, 2H); MS (ESI(+)) m/e 395 (M+H)⁺.

Example 464N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[6-(morpholin-4-yl)pyridin-3-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting4-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)morpholinefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.34 (t, J=6.0 Hz,1H), 8.87 (d, J=7.0 Hz, 1H), 8.51 (d, J=2.5 Hz, 1H), 8.33 (d, J=2.2 Hz,1H), 8.15 (d, J=2.1 Hz, 1H), 7.90 (dd, J=8.9, 2.6 Hz, 1H), 7.85 (d,J=3.9 Hz, 1H), 7.81 (s, 1H), 7.50-7.44 (m, 2H), 6.94 (d, J=9.0 Hz, 1H),4.67 (d, J=5.9 Hz, 2H), 3.75-3.66 (m, 4H), 3.57-3.49 (m, 4H); MS(ESI(+)) m/e 420 (M+H).

Example 467N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamideExample 467A tert-butyl3-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(1-(tert-butoxycarbonyl)pyrrolidin-3-yl)thiophene-2-carboxylic acidfor 4-nitrobenzoic acid.

Example 467BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(pyrrolidin-3-yl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 467CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(pyrrolidin-3-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.02 (t, J=5.4 Hz, 1H), 8.48 (d,J=6.8 Hz, 1H), 7.88 (s, 1H), 7.68 (dd, J=3.9, 2.2 Hz, 1H), 7.52 (d,J=1.4 Hz, 1H), 7.37 (s, 1H), 7.02 (dd, J=8.1, 3.7 Hz, 1H), 6.82 (dd,J=7.0, 1.5 Hz, 1H), 4.46 (d, J=5.8 Hz, 2H), 3.22-3.94 (m, 5H), 2.21-2.42(m, 1H), 2.10-2.17 (m, 2H), 1.86-2.09 (m, 2H), 0.86-0.95 (m, 6H); MS(ESI(+)) m/e 411 (M+H)⁺.

TABLE 23 The following Examples were prepared essentially as describedin Example 467, using an appropriate carboxylic acid in Example 467C. ExName MS 540 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3- (ESI(+))trifluoropropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 437 (M +H)⁺ 541 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2- (ESI(+))methylpropanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 397 (M + H)⁺542 5-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)thiophene-2-carboxamide m/e 431 (M + H)⁺ 7175-[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 395 (M + H)⁺ 718N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4- (ESI(+))methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 445 (M + H)⁺756 5-[1-(cyclopropylacetyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 409 (M + H)⁺ 7575-[1-(2-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 465 (M + H)⁺ 7585-{1-[(4-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 463 (M + H)⁺ 759N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3- (ESI(+))methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 461 (M + H)⁺760 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2- (ESI(+))methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 461 (M + H)⁺761 5-{1-[(3-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 463 (M + H)⁺762 5-[1-(3-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 449 (M + H)⁺ 7635-[1-(4-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 449 (M + H)⁺ 7645-{1-[(3,5-difluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 481 (M + H)⁺765 5-{1-[(2-fluorophenyl)acetyl]pyrrolidin-3-yl}-N-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 463 (M + H)⁺766 5-[1-(4-cyanobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 456 (M + H)⁺ 767N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methyloxetan-3- (ESI(+))yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide m/e 425 (M + H)⁺ 7685-[1-(3,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)thiophene-2-carboxamide m/e 467 (M + H)⁺ 7695-[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 421 (M + H)⁺ 7705-[1-(4-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 465 (M + H)⁺ 771N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrro1-2-(ESI(+)) yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide m/e 434(M + H)⁺ 7725-[1-(2,4-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)thiophene-2-carboxamide m/e 467 (M + H)⁺ 773N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-4- (ESI(+))ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 432 (M + H)⁺ 774N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-2- (ESI(+))ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 432 (M + H)⁺ 775N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-(ESI(+)) 4-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide m/e 435(M + H)⁺ 7765-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 449 (M + H)⁺ 777N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2E)-2-methylpent-2- (ESI(+))enoyl]pyrrolidin-3-yl}thiophene-2-carboxamide m/e 423 (M + H)⁺ 7785-{1-[(2,5-dimethylfuran-3-yl)carbonyl]pyrrolidin-3-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 449 (M +H)⁺ 7795-[1-(3-chlorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 465 (M + H)⁺ 780N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-propanoylpyrrolidin-3-(ESI(+)) yl)thiophene-2-carboxamide m/e 383 (M + H)⁺ 7815-{1-[(1-cyanocyclopropyl)carbonyl]pyrrolidin-3-yl}-N- (ESI(+))(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 420 (M +H)⁺ 782 5-(1-butanoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)thiophene-2-carboxamide m/e 397 (M + H)⁺ 7835-[1-(furan-2-ylcarbonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)thiophene-2-carboxamide m/e 421 (M + H)⁺ 784N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4- (ESI(+))methoxybenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 461 (M + H)⁺785 5-[1-(2,5-difluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)thiophene-2-carboxamide m/e 467 (M + H)⁺ 786N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(thiophen-2- (ESI(+))ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 437 (M + H)⁺ 7875-[1-(2,2-dimethylpropanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 411 (M + H)⁺ 7885-[1-(3, 3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 425 (M + H)⁺ 7915-[1-(2,2-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 425 (M + H)⁺ 792N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyrazin-2- (ESI(+))ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 433 (M + H)⁺ 793N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylthiophen-2- (ESI(+))yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide m/e 451 (M + H)⁺ 794N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2- (ESI(+))methylbenzoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 445 (M + H)⁺795 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1- (ESI(+))methylcyclopropyl)carbonyl]pyrrolidin-3-yl}thiophene-2- m/e 409carboxamide (M + H)⁺ 796N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4- (ESI(+))trifluorobutanoyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 451 (M +H)⁺ 797 5-{1-[(3,5-dimethyl-1,2-oxazo1-4-yl)carbonyl]pyrrolidin-3-yl}-N-(ESI(+)) (imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e450 (M + H)⁺ 798 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(pyridin-3-(ESI(+)) ylcarbonyl)pyrrolidin-3-yl]thiophene-2-carboxamide m/e 432 (M +H)⁺ 799 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(1-methyl-1H-pyrazol-(ESI(+)) 5-yl)carbonyl]pyrrolidin-3-yl}thiophene-2-carboxamide m/e 435(M + H)⁺ 800 5-[1-(2,3-dimethylbutanoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)thiophene-2-carboxamide m/e 425 (M + H)⁺

Example 468N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropanoyl)amino]cyclobutyl}thiophene-2-carboxamideExample 468A5-(1-(1,1-dimethylethylsulfinamido)cyclobutyl)thiophene-2-carboxylicacid

The title compound was prepared as described in Example 324A,substituting N-cyclobutylidene-2-methylpropane-2-sulfinamide forN-(oxetan-3-ylidene)propane-2-sulfinamide.

Example 468B5-(1-(1,1-dimethylethylsulfinamido)cyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(1-(1,1-dimethylethylsulfinamido)cyclobutyl)thiophene-2-carboxylicacid for 4-nitrobenzoic acid.

Example 468C5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared in Example 324C, substituting5-(1-(1,1-dimethylethylsulfinamido)cyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor5-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide.

Example 468D

The title compound was prepared as described in Example 1A, substituting5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.97 (t, J=5.9 Hz, 1H), 8.53 (s, 1H),8.48 (d, J=7.1 Hz, 1H), 7.88 (s, 1H), 7.63 (d, J=3.7 Hz, 1H), 7.52 (d,J=1.4 Hz, 1H), 7.38 (s, 1H), 7.04 (d, J=3.7 Hz, 1H), 6.82 (dd, J=6.8,1.7 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 2.36-2.48 (m, 5H), 1.86-2.01 (m,2H), 0.99 (d, J=6.8 Hz, 6H); MS (ESI(+)) m/e 397 (M+H)⁺.

Example 469N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3-methylbutanoyl)amino]cyclobutyl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.97 (t, J=5.9 Hz, 1H), 8.59 (s,1H), 8.48 (d, J=7.8 Hz, 1H), 7.88 (s, 1H), 7.63 (d, J=4.1 Hz, 1H), 7.51(d, J=1.0 Hz, 1H), 7.37 (s, 1H), 7.05 (d, J=3.7 Hz, 1H), 6.82 (dd,J=7.1, 1.7 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 2.39-2.47 (m, 4H), 1.83-2.03(m, 5H), 0.87 (d, J=6.4 Hz, 6H); MS (ESI(+)) m/e 411 (M+H)⁺.

Example 470N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1-{[(2S)-2-methylbutanoyl]amino}cyclobutyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.97 (t, J=6.1 Hz,1H), 8.57 (s, 1H), 8.47 (d, J=7.1 Hz, 1H), 7.88 (s, 1H), 7.63 (d, J=4.1Hz, 1H), 7.51 (d, J=1.4 Hz, 1H), 7.37 (s, 1H), 7.04 (d, J=3.7 Hz, 1H),6.82 (dd, J=7.0, 1.5 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 2.37-2.49 (m, 4H),2.13-2.26 (m, 1H), 1.84-2.01 (m, 2H), 1.40-1.59 (m, 1H), 1.20-1.36 (m,1H), 0.97 (d, J=6.8 Hz, 3H), 0.82 (t, J=7.3 Hz, 3H); MS (ESI(+)) m/e 411(M+H)⁺.

Example 4715-[1-(benzoylamino)cyclobutyl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.17 (s, 1H), 8.98 (t, J=5.9 Hz, 1H), 8.46(d, J=6.1 Hz, 1H), 7.84-7.90 (m, 3H), 7.65 (d, J=4.1 Hz, 1H), 7.43-7.57(m, 4H), 7.37 (s, 1H), 7.14 (d, J=4.1 Hz, 1H), 6.81 (dd, J=6.8, 1.7 Hz,1H), 4.44 (d, J=6.1 Hz, 2H), 2.61-2.73 (m, 2H), 2.50-2.60 (m, 2H),1.91-2.07 (m, 2H); MS (ESI(+)) m/e 431 (M+H)⁺.

Example 472N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3,3,3-trifluoropropanoyl)amino]cyclobutyl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3,3,3-trifluoropropanoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.08 (s, 1H), 9.00(t, J=5.9 Hz, 1H), 8.48 (d, J=7.8 Hz, 1H), 7.88 (s, 1H), 7.65 (d, J=3.7Hz, 1H), 7.52 (s, 1H), 7.38 (s, 1H), 7.07 (d, J=3.7 Hz, 1H), 6.83 (dd,J=6.8, 1.7 Hz, 1H), 4.46 (d, J=5.8 Hz, 2H), 3.19-3.36 (m, 2H), 2.43-2.53(m, 4H), 1.86-2.03 (m, 2H); MS (ESI(+)) m/e 437 (M+H)⁺.

Example 473N-(1-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}cyclobutyl)tetrahydro-2H-pyran-4-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(1-aminocyclobutyl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and tetrahydro-2H-pyran-4-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.97 (t, J=6.1 Hz,1H), 8.60 (s, 1H), 8.48 (d, J=7.1 Hz, 1H), 7.88 (s, 1H), 7.63 (d, J=3.7Hz, 1H), 7.51 (d, J=1.0 Hz, 1H), 7.37 (s, 1H), 7.04 (d, J=3.7 Hz, 1H),6.82 (dd, J=7.0, 1.5 Hz, 1H), 4.45 (d, J=5.8 Hz, 2H), 3.81-3.89 (m, 2H),3.24-3.36 (m, 2H), 2.33-2.48 (m, 5H), 1.84-2.00 (m, 2H), 1.47-1.65 (m,4H); MS (ESI(+)) m/e 439 (M+H)⁺.

Example 474 tert-butyl3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}azetidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)azetidin-3-yloxy)benzoic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.98 (t, J=5.9 Hz,1H), 8.48 (d, J=7.0 Hz, 1H), 7.89 (m, 3H), 7.51 (d, J=1.1 Hz, 1H), 7.37(s, 1H), 6.92 (m, 2H), 6.84 (dd, J=7.0, 1.6 Hz, 1H), 5.06 (m, 1H), 4.49(d, J=5.9 Hz, 2H), 4.33 (m, 2H), 3.80 (m, 2H), 1.39 (s, 9H); MS (ESI(+))m/e 423 (M+H)⁺.

Example 485N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(piperidin-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamideExample 485A tert-butyl4-((4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)thiophen-2-yl)-1H-pyrazol-1-yl)methyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)methyl)piperidine-1-carboxylatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline.

Example 485BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(piperidin-4-ylmethyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-((4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)thiophen-2-yl)-1H-pyrazol-1-yl)methyl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.¹H NMR (300 MHz, methanol-d₄) δ 8.76 (dd, J=7.1, 0.9 Hz, 1H), 8.19 (dd,J=2.2, 0.7 Hz, 1H), 8.07 (s, 1H), 8.00 (d, J=2.2 Hz, 1H), 7.83 (d, J=0.6Hz, 2H), 7.72 (d, J=3.8 Hz, 1H), 7.49 (dd, J=7.0, 1.6 Hz, 1H), 7.22 (d,J=3.9 Hz, 1H), 4.75 (s, 2H), 4.15 (d, J=7.0 Hz, 2H), 3.48-3.36 (m, 2H),3.08-2.91 (m, 2H), 2.37-2.15 (m, 1H), 1.85 (d, J=14.0 Hz, 2H), 1.63-1.43(m, 2H); MS (ESI(+)) m/e 421 (M+H)⁺.

Example 4861-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}ureaExample 486A 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

To a solution of imidazo[1,2-a]pyridin-7-ylmethanamine (500 mg, 3.40mmol) in dichloromethane (17 ml) at room temperature was added1-bromo-4-isocyanatobenzene (680 mg, 3.40 mmol) as a single portion. Theresulting suspension was stirred overnight and then filtered withdichloromethane washes to give the title compound.

Example 486B1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methylpropyl)-1H-pyrazol-4-yl]phenyl}urea

The title compound was prepared as described in Example 51A,substituting substituting1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor 1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.62 (s, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 8.02 (d, J=0.8 Hz, 1H), 7.88 (dd, J=1.2, 0.7 Hz,1H), 7.77 (d, J=0.8 Hz, 1H), 7.54-7.34 (m, 6H), 6.84 (dd, J=7.0, 1.7 Hz,1H), 6.69 (t, J=6.0 Hz, 1H), 4.34 (d, J=5.9 Hz, 2H), 3.90 (d, J=7.1 Hz,2H), 2.21-2.04 (m, 1H), 0.86 (d, J=6.7 Hz, 6H). MS (ESI(+)) m/e 389(M+H)⁺.

Example 4871-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]urea

The title compound was prepared as described in Example 51A,substituting1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (s, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 8.04 (d, J=0.8 Hz, 1H), 7.90-7.86 (m, 1H), 7.76 (d,J=0.8 Hz, 1H), 7.51 (d, J=1.2 Hz, 1H), 7.46-7.35 (m, 5H), 6.84 (dd,J=7.0, 1.7 Hz, 1H), 6.69 (t, J=6.0 Hz, 1H), 4.34 (d, J⁼5.9 Hz, 2H), 4.04(t, J⁼6.9 Hz, 2H), 1.91-1.73 (m, 2H), 1.26-1.05 (m, 1H), 0.85 (t, J=7.4Hz, 3H); MS (ESI(+)) m/e 375 (M+H)⁺.

Example 489 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-phenoxybenzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-phenoxybenzoic acid for 4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆)δ ppm 9.05 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9, 0.9 Hz, 1H), 7.95 (m,2H), 7.89 (s, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.44 (m, 2H), 7.38 (s, 1H),7.22 (m, 1H), 7.14-6.98 (m, 4H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 4.50 (d,J=5.9 Hz, 2H); MS (ESI(+)) m/e 344 (M+H)⁺.

Example 490N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)azetidin-3-yl]benzamideExample 490A4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}azetidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 490BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpropanoyl)azetidin-3-yl]benzamide

The title compound was prepared as described in Example 1A, substituting-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for3-methylbutan-1-amine and 2-methylpropanoic acid for 4-nitrobenzoicacid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.10 (t, J=5.9 Hz, 1H), 8.48 (d,J=7.0 Hz, 1H), 7.91 (m, 3H), 7.52 (d, J=1.0 Hz, 1H), 7.48 (m, 2H), 7.38(s, 1H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 4.58 (t, J=8.6 Hz, 1H), 4.51 (d,J=5.9 Hz, 2H), 4.26 (t, J=9.0 Hz, 1H), 4.18 (dd, J=8.4, 6.0 Hz, 1H),3.92 (m, 1H), 3.84 (m, 1H), 3.17 (d, J=5.0 Hz, 1H), 1.00 (dd, J=6.8, 1.6Hz, 6H); MS (ESI(+)) m/e 377 (M+H)⁺.

TABLE 24 The following Examples were prepared essentially as describedin Example 490, using an appropriate carboxylic acid in Example 490B. ExName MS 547 N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2S)-2- (ESI(+))methylbutanoyl]azetidin-3-yl}benzamide m/e 391 (M + H)⁺ 5484-[1-(cyclopropylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 389 (M + H)⁺ 5494-(1-benzoylazetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 411 (M + H)⁺ 5504-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-(ESI(+)) a]pyridin-7-ylmethyl)benzamide m/e 393 (M + H)⁺ 551N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(tetrahydro-2H-pyran-4-(ESI(+)) ylacetyl)azetidin-3-yl]benzamide m/e 433 (M + H)⁺ 552N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-2- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 417 (M + H)⁺ 628N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(2- (ESI(+))methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide m/e 389 (M + H)⁺ 6294-[1-(cyclopentylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 417 (M + H)⁺ 630N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- (ESI(+))methylpentanoyl)azetidin-3-yl]benzamide m/e 405 (M + H)⁺ 6314-[1-(cyclopentylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 403 (M + H)⁺ 632N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1- (ESI(+))methylcyclopropyl)carbonyl]azetidin-3-yl}benzamide m/e 389 (M + H)⁺ 6334-[1-(2,2-dimethylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2- (ESI(+))a]pyridin-7-ylmethyl)benzamide m/e 391 (M + H)⁺ 634N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazo1-5- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 418 (M + H)⁺ 635N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrazin-2- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 413 (M + H)⁺ 636N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- (ESI(+))methoxybenzoyl)azetidin-3-yl]benzamide m/e 441 (M + H)⁺ 637N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazo1-4- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 418 (M + H)⁺ 6384-[1-(2-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 429 (M + H)⁺ 6394-[1-(furan-2-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 401 (M + H)⁺ 6404-[1-(3-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 429 (M + H)⁺ 6414-[1-(2,4-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 447 (M + H)⁺ 642N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrazol-(ESI(+)) 3-yl)carbonyl]azetidin-3-yl}benzamide m/e 415 (M + H)⁺ 6434-[1-(2-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 445 (M + H)⁺ 644N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2- (ESI(+))methylbenzoyl)azetidin-3-yl]benzamide m/e 425 (M + H)⁺ 6454-[1-(4-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 445 (M + H)⁺ 6464-[1-(3-chlorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 445 (M + H)⁺ 6474-[1-(2,2-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 405 (M + H)⁺ 6484-[1-(3,5-difluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 447 (M + H)⁺ 6494-[1-(4-fluorobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 429 (M + H)⁺ 650N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4- (ESI(+))methylbenzoyl)azetidin-3-yl]benzamide m/e 425 (M + H)⁺ 651N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- (ESI(+))methylbutanoyl)azetidin-3-yl]benzamide m/e 391 (M + H)⁺ 6524-[1-(3,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 405 (M + H)⁺ 6534-[1-(3-cyanobenzoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7- (ESI(+))ylmethyl)benzamide m/e 436 (M + H)⁺ 654N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- (ESI(+))methoxybenzoyl)azetidin-3-yl]benzamide m/e 441 (M + H)⁺ 655N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(4- (ESI(+))methoxybenzoyl)azetidin-3-yl]benzamide m/e 441 (M + H)⁺ 565N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1-methyl-1H-pyrrol-2-(ESI(+)) yl)carbonyl]azetidin-3-yl}benzamide m/e 414 (M + H)⁺ 6574-[1-(cyclohexylacetyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 431 (M + H)⁺ 658N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-4- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 412 (M + H)⁺ 659N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-3- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 412 (M + H)⁺ 6604-[1-(cyclohexylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 417 (M + H)⁺ 661N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyridin-2- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 412 (M + H)⁺ 6624-[1-(furan-3-ylcarbonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-(ESI(+)) ylmethyl)benzamide m/e 401 (M + H)⁺ 663N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 413 (M + H)⁺ 664N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(1,3-thiazol-2- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 418 (M + H)⁺ 665N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(1- (ESI(+))methylcyclohexyl)carbonyl]azetidin-3-yl} benzamide m/e 431 (M + H)⁺ 6664-[1-(2,3-dimethylbutanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-(ESI(+)) 7-ylmethyl)benzamide m/e 405 (M + H)⁺ 667N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(3- (ESI(+))methylbenzoyl)azetidin-3-yl]benzamide m/e 425 (M + H)⁺ 668N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(thiophen-3- (ESI(+))ylcarbonyl)azetidin-3-yl]benzamide m/e 417 (M + H)⁺ 669N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3- (ESI(+))(trifluoromethoxy)benzoyl]azetidin-3-yl}benzamide m/e 495 (M + H)⁺ 670N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[(3-methylthiophen-2- (ESI(+))yl)carbonyl]azetidin-3-yl}benzamide m/e 431 (M + H)⁺ 671N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[3- (ESI(+))(trifluoromethyl)benzoyl]azetidin-3-yl}benzamide m/e 479 (M + H)⁺

Example 491 tert-butyl4-{4-[(3-chloroimidazo[1,2-a]pyridin-6-yl)carbamoyl]phenyl}piperidine-1-carboxylate

A solution of tert-butyl4-(4-(imidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl)piperidine-1-carboxylate(0.015 g, 0.036 mmol) in chloroform (0.618 ml) and methanol (0.095 ml)was treated with N-chlorosuccinimide (5.24 mg, 0.039 mmol) and thereaction was stirred at ambient temperature for 16 hours. The reactionmixture was concentrated under a stream of warm nitrogen. The residuewas purified by normal phase flash chromatography to provide the titlecompound. ¹H NMR (500 MHz, methanol-d₄) δ ppm 9.23 (s, 1H), 7.93 (d,J=8.3 Hz, 2H), 7.62-7.51 (m, 3H), 7.42 (d, J=8.3 Hz, 2H), 4.27-4.19 (m,2H), 2.96-2.76 (m, 3H), 1.90-1.82 (m, 2H), 1.70-1.57 (m, 2H), 1.48 (s,9H); MS (ESI(+)) m/e 455 (M+H)⁺.

Example 492N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamideExample 492A(R)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl(3R)-3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 492BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(3R)-1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}benzamide

The title compound was prepared as described in Example 1A, substituting(R)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (500 MHz, methanol-d₄) δ ppm 8.75 (d, J=7.0 Hz, 1H), 8.17 (d,J=2.2 Hz, 1H), 7.99 (d, J=2.2 Hz, 1H), 7.94-7.86 (m, 2H), 7.80 (bs, 1H),7.48 (dd, J=7.0, 1.6 Hz, 1H), 7.11-7.01 (m, 2H), 5.23-5.11 (m, 1H), 4.76(s, 2H), 3.92-3.47 (m, 4H), 2.87-2.64 (m, 1H), 2.36-2.16 (m, 2H),1.16-1.01 (m, 6H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 4934-{[(3R)-1-benzoylpyrrolidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substituting(R)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, methanol-d₄) δ ppm 8.74 (t, J=6.6 Hz, 1H), 8.20-8.14 (m,1H), 8.01-7.96 (m, 1H), 7.92 (d, J=8.7 Hz, 1H), 7.85 (d, J=8.6 Hz, 1H),7.82-7.76 (m, 1H), 7.59-7.39 (m, 6H), 7.10 (d, J=8.6 Hz, 1H), 7.00 (d,J=8.6 Hz, 1H), 5.24-5.07 (m, 1H), 4.75 (d, J=12.3 Hz, 2H), 3.99-3.70 (m,3H), 3.66-3.56 (m, 1H), 2.39-2.19 (m, 2H); MS (ESI(+)) m/e 441 (M+H)⁺.

Example 494N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(3S)-tetrahydrofuran-3-ylcarbonyl]pyrrolidin-3-yl}oxy)benzamide

The title compound was prepared as described in Example 1A, substituting(R)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamidefor 3-methylbutan-1-amine and (S)-tetrahydrofuran-3-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, methanol-d₄) δ ppm 8.75 (d, J=7.0Hz, 1H), 8.19-8.15 (m, 1H), 8.01-7.97 (m, 1H), 7.93-7.86 (m, 2H),7.82-7.77 (m, 1H), 7.51-7.45 (m, 1H), 7.10-7.01 (m, 2H), 5.23-5.12 (m,1H), 4.75 (s, 2H), 4.05-3.92 (m, 1H), 3.94-3.63 (m, 7H), 3.57-3.34 (m,1H), 2.40-2.29 (m, 1H), 2.27-1.97 (m, 3H); MS (ESI(+)) m/e 435 (M+H)⁺.

Example 495N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({(3R)-1-[(2S)-2-methylbutanoyl]pyrrolidin-3-yl}oxy)benzamide

The title compound was prepared as described in Example 1A, substituting(R)—N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yloxy)benzamidefor 3-methylbutan-1-amine and (S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, methanol-d₄) δ ppm 8.75 (d, J=7.0Hz, 1H), 8.17 (d, J=2.2 Hz, 1H), 7.99 (d, J=2.2 Hz, 1H), 7.94-7.86 (m,2H), 7.82-7.77 (m, 1H), 7.48 (d, J=7.1 Hz, 1H), 7.10-7.00 (m, 2H),5.22-5.11 (m, 1H), 4.76 (s, 2H), 3.91-3.49 (m, 4H), 2.70-2.49 (m, 1H),2.35-2.17 (m, 2H), 1.73-1.59 (m, 1H), 1.50-1.36 (m, 1H), 1.14-1.03 (m,3H), 0.93-0.86 (m, 3H); MS (ESI(+)) m/e 421 (M+H)⁺.

Example 496 1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-phenoxyphenyl)urea

The title compound was prepared as described in Example 1C, substituting4-phenoxyaniline for 4-amino-N-isopentylbenzamide andimidazo[1,2-a]pyridin-7-ylmethanamine for imidazo[1,2-a]pyridin-6-amine.¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.68 (s, 1H), 8.49 (dd, J=6.9, 0.9 Hz,1H), 7.88 (t, J=0.9 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.44 (m, 2H), 7.39(m, 1H), 7.34 (m, 2H), 7.07 (m, 1H), 6.93 (m, 4H), 6.84 (dd, J=7.0, 1.7Hz, 1H), 6.70 (t, J=6.0 Hz, 1H), 4.34 (d, J=6.0 Hz, 2H); MS (ESI(+)) m/e359 (M+H)⁺.

Example 4975-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 497A 5-(1-isobutyl-1H-pyrazol-4-yl)thiophene-2-carboxylic acid

The title compound was prepared as described in Example 51A,substituting 5-bromothiophene-2-carboxylic acid for 4-bromoaniline.

Example 497B5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amineand 5-(1-isobutyl-1H-pyrazol-4-yl)thiophene-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.11 (t, J=6.0 Hz,1H), 8.90 (dd, J=7.1, 1.0 Hz, 1H), 8.46 (s, 1H), 8.15 (d, J=0.9 Hz, 1H),7.81 (s, 1H), 7.75 (d, J=3.9 Hz, 1H), 7.71-7.64 (m, 1H), 7.23 (d, J=3.8Hz, 1H), 7.16 (dd, J=7.1, 1.8 Hz, 1H), 4.58 (d, J=5.8 Hz, 2H), 3.93 (d,J=7.1 Hz, 2H), 2.20-2.04 (m, 1H), 0.86 (d, J=6.6 Hz, 6H); MS (ESI(+))m/e 381 (M+H)⁺.

Example 543N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamideExample 543A2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and2-bromothiazole-5-carboxylic acid for 4-nitrobenzoic acid.

Example 543B tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)thiazol-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 2-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiazole-5-carboxamidefor 4-bromoaniline.

Example 543C tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)thiazol-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1B, substitutingtert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)thiazol-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor N-isopentyl-4-nitrobenzamide.

Example 543DN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(piperidin-4-yl)thiazole-5-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)thiazol-2-yl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 543EN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(piperidin-4-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.23 (t, J=6.0 Hz, 1H), 8.49 (d, J=7.0Hz, 1H), 8.33 (s, 1H), 7.89 (bs, 1H), 7.52 (d, J=1.0 Hz, 1H), 7.40 (bs,1H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 4.48 (d, J=6.1 Hz, 2H), 4.44 (d,J=13.4 Hz, 1H), 4.02 (d, J=13.1 Hz, 1H), 3.34-3.27 (m, 1H), 3.19 (t,J=11.9 Hz, 1H), 2.95-2.84 (m, 1H), 2.72 (t, J=12.1 Hz, 1H), 2.13-2.02(m, 2H), 1.68-1.43 (m, 2H), 1.04-0.96 (m, 6H); MS (ESI(+)) m/e 412(M+H)⁺.

Example 544N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)piperidin-4-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(piperidin-4-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ππμ9.23 (t, J=5.9 Hz, 1H), 8.49 (dd,J=6.9, 0.9 Hz, 1H), 8.33 (s, 1H), 7.92-7.87 (m, 1H), 7.53 (d, J=1.2 Hz,1H), 7.40 (d, J=1.6 Hz, 1H), 6.84 (dd, J=6.9, 1.7 Hz, 1H), 4.51-4.41 (m,3H), 3.96 (d, J=13.8 Hz, 1H), 3.34-3.24 (m, 1H), 3.16 (t, J=11.7 Hz,1H), 2.71 (t, J=12.2 Hz, 1H), 2.21 (dd, J=7.0, 2.3 Hz, 2H), 2.10-2.00(m, 2H), 1.61 (qd, J=12.7, 4.3 Hz, 1H), 1.49 (qd, J=12.5, 4.4 Hz, 1H),0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 426 (M+H)⁺.

Example 5452-(1-benzoylpiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(piperidin-4-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, DMSO-d₆) δ ppm 9.24 (t, J=5.9 Hz, 1H), 8.49 (d, J=7.0 Hz,1H), 8.34 (s, 1H), 7.89 (s, 1H), 7.53 (d, J=1.1 Hz, 1H), 7.43 (ddd,J=9.6, 6.8, 3.7 Hz, 6H), 6.84 (dd, J=7.0, 1.6 Hz, 1H), 4.48 (d, J=5.9Hz, 2H), 4.48 (d, J=5.9 Hz, 1H), 3.72-3.58 (m, 1H), 3.26-3.13 (m, 1H),3.06-2.91 (m, 1H), 2.17-1.95 (m, 2H), 1.72-1.62 (m, 2H); MS (ESI(+)) m/e446 (M+H)⁺.

Example 5464-[(cyclopentylacetyl)amino]-N-([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amineand 4-(2-cyclopentylacetamido)benzoic acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, methanol-d₄) δ ppm 8.78-8.72 (m, 1H), 8.40 (s, 1H),7.90-7.83 (m, 2H), 7.75-7.67 (m, 3H), 7.25 (dd, J=7.0, 1.8 Hz, 1H),4.75-4.69 (m, 2H), 2.44-2.25 (m, 3H), 1.95-1.76 (m, 2H), 1.78-1.50 (m,4H), 1.35-1.17 (m, 2H); MS (ESI(+)) m/e 378 (M+H)⁺.

Example 5535-[4-hydroxy-1-(3-methylbutanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 553A5-(4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-hydroxy-4-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophen-2-yl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 553B5-[3-hydroxy-1-(2-methylpropanoyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 2-methylpropanoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.98 (t, J=6.0 Hz, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.90-7.87 (m, 1H), 7.65 (d, J=3.8 Hz, 1H), 7.51 (d,J=1.2 Hz, 1H), 7.37 (s, 1H), 7.00 (d, J=3.8 Hz, 1H), 6.83 (dd, J=7.0,1.7 Hz, 1H), 5.76 (s, 1H), 4.46 (d, J=5.9 Hz, 2H), 4.33-4.23 (m, 1H),3.81-3.71 (m, 1H), 2.99-2.85 (m, 1H), 2.21 (d, J=7.0 Hz, 2H), 2.07-1.91(m, 1H), 1.86-1.71 (m, 4H), 0.94-0.87 (m, 6H); MS (ESI(+)) m/e 441(M+H)⁺.

Example 5545-[4-hydroxy-1-(2-methylpropanoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.98 (s, 1H), 8.48 (d, J=7.0 Hz, 1H),7.88 (s, 1H), 7.65 (d, J=3.8 Hz, 1H), 7.51 (d, J=1.1 Hz, 1H), 7.37 (s,1H), 7.01 (d, J=3.8 Hz, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 5.77 (s, 1H),4.46 (d, J=5.6 Hz, 2H), 4.33-4.22 (m, 1H), 3.88-3.74 (m, 1H), 2.98-2.82(m, 2H), 1.82 (s, 4H), 1.05-0.96 (m, 6H); MS (ESI(+)) m/e 427 (M+H)⁺.

Example 5555-[1-(3,3-dimethylbutanoyl)-4-hydroxypiperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3,3-dimethylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.98 (t, J=5.8 Hz,1H), 8.48 (dd, J=6.9, 0.9 Hz, 1H), 7.91-7.86 (m, 1H), 7.65 (d, J=3.8 Hz,1H), 7.52 (d, J=1.2 Hz, 1H), 7.37 (s, 1H), 7.00 (d, J=3.8 Hz, 1H), 6.83(dd, J=7.0, 1.7 Hz, 1H), 5.76 (s, 1H), 4.46 (d, J=6.0 Hz, 2H), 4.38-4.28(m, 1H), 3.89-3.78 (m, 1H), 2.97-2.85 (m, 1H), 2.38-2.13 (m, 3H),1.86-1.71 (m, 4H), 0.99 (s, 9H); MS (ESI(+)) m/e 455 (M+H)⁺.

Example 5565-(1-benzoyl-4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting5-(4-hydroxypiperidin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 8.98 (s, 1H), 8.48 (d, J=6.2 Hz, 1H), 7.88(s, 1H), 7.66 (d, J=3.8 Hz, 1H), 7.53-7.35 (m, 7H), 7.06 (d, J=3.8 Hz,1H), 6.83 (d, J=7.0 Hz, 1H), 5.83 (s, 1H), 4.46 (d, J=5.9 Hz, 3H),4.52-4.26 (m, 1H), 1.93 (s, 5H); MS (ESI(+)) m/e 461 (M+H)⁺.

Example 557N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)azetidin-3-yl]benzamideExample 557A tert-butyl3-(4-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)phenyl)azetidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)azetidin-3-yl)benzoic acid for 4-nitrobenzoicacid.

Example 557B4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-(4-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)phenyl)azetidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 557CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)azetidin-3-yl]benzamide

In a 4 mL vial was mixed4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamidebis(2,2,2-trifluoroacetate) (60 mg, 0.112 mmol) in anhydroustetrahydrofuran (2 mL) at room temperature. To this mixture was added inportions 60% sodium hydride in mineral oil (22.45 mg, 0.561 mmol). Thisheterogeneous mixture was stirred 1 hour. To this was addedpropane-2-sulfonyl chloride (0.015 mL, 0.135 mmol) at and reactionmixture was stirred for 3 hours. The mixture was quenched with water,and product was extracted with 10% methanol/dichloromethane. The organiclayers were combined, concentrated and purified by normal phasechromatography to give the title compound. ¹H NMR (400 MHz, DMSO-d₆) δppm 9.07 (m, 1H), 8.47 (d, J=7.0 Hz, 1H), 7.90 (m, 3H), 7.48 (m, 3H),7.37 (s, 1H), 6.84 (m, 1H), 4.50 (d, J=5.9 Hz, 2H), 4.22 (m, 2H), 3.93(m, 3H), 3.48 (m, 1H), 1.25 (d, J=5.9 Hz, 6H); MS (ESI(+)) m/e 413(M+H)⁺.

Example 558N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}benzamideExample 558A4-(azetidin-3-yloxy)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenoxy}azetidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 558BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[1-(2-methylpropanoyl)azetidin-3-yl]oxy}benzamide

The title compound was prepared as described in Example 1A, substituting4-(azetidin-3-yloxy)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 8.99 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9,0.9 Hz, 1H), 7.90 (m, 3H), 7.51 (d, J=1.2 Hz, 1H), 7.37 (m, 1H), 6.95(m, 2H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 5.11 (m, 1H), 4.64 (dd, J=9.5,6.4 Hz, 1H), 4.49 (d, J=5.8 Hz, 2H), 4.32 (dd, J=10.4, 6.3 Hz, 1H), 4.09(m, 1H), 3.78 (dd, J=10.6, 3.9 Hz, 1H), 2.48 (m, 1H), 0.98 (t, J=6.7 Hz,6H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 559N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-({1-[(2S)-2-methylbutanoyl]azetidin-3-yl}oxy)benzamide

The title compound was prepared as described in Example 1A, substituting4-(azetidin-3-yloxy)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for3-methylbutan-1-amine and (2S)-2-methylbutyric acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.99 (t, J=5.9 Hz, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.90 (m, 3H), 7.51 (d, J=1.2 Hz, 1H), 7.37 (s, 1H),6.95 (m, 2H), 6.85 (dd, J=6.9, 1.6 Hz, 1H), 5.11 (dd, J=6.4, 3.5 Hz,1H), 4.63 (dd, J=9.5, 6.5 Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.33 (m, 1H),4.11 (m, 1H), 3.79 (m, 1H), 2.29 (m, 1H), 1.50 (m, 1H), 1.28 (m, 1H),0.97 (t, J=6.0 Hz, 3H), 0.82 (m, 3H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 5604-{[1-(cyclopropylacetyl)azetidin-3-yl]oxy}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substituting4-(azetidin-3-yloxy)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for3-methylbutan-1-amine and cyclopropylacetic acid for 4-nitrobenzoicacid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.99 (t, J=5.9 Hz, 1H), 8.48 (dd,J=6.9, 0.9 Hz, 1H), 7.90 (m, 3H), 7.51 (d, J=1.2 Hz, 1H), 7.37 (s, 1H),6.94 (m, 2H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 5.10 (m, 1H), 4.57 (dd,J=9.5, 6.5 Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.33 (dd, J=10.6, 6.5 Hz,1H), 4.08 (dd, J=9.6, 3.8 Hz, 1H), 3.78 (dd, J=10.6, 3.9 Hz, 1H), 2.03(d, J=6.8 Hz, 2H), 0.91 (m, 1H), 0.44 (m, 2H), 0.10 (m, 2H); MS (ESI(+))m/e 405 (M+H)⁺.

Example 5614-[(1-benzoylazetidin-3-yl)oxy]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substituting4-(azetidin-3-yloxy)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 8.99 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9, 0.9Hz, 1H), 7.90 (m, 3H), 7.66 (m, 2H), 7.59-7.42 (m, 4H), 7.37 (s, 1H),6.95 (m, 2H), 6.84 (dd, J=6.9, 1.7 Hz, 1H), 5.17 (m, 1H), 4.71 (m, 1H),4.57 (m, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.33 (m, 1H), 4.02 (m, 1H); MS(ESI(+)) m/e 427 (M+H)⁺.

Example 563 tert-butyl4-{4-[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amineand 4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.11 (t, J=5.9 Hz,1H), 8.89 (dd, J=7.0, 0.9 Hz, 1H), 8.44 (s, 1H), 7.89-7.83 (m, 2H),7.67-7.65 (m, 1H), 7.40-7.34 (m, 2H), 7.15 (dd, J=7.0, 1.8 Hz, 1H),4.62-4.57 (m, 2H), 4.14-4.03 (m, 2H), 2.91-2.67 (m, 3H), 1.82-1.71 (m,2H), 1.60-1.37 (m, 11H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 5642-cyclopentyl-N-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)acetamide

The title compound was prepared as described in Example 1C, substitutingN-(4-aminophenyl)-2-cyclopentylacetamide for4-amino-N-isopentylbenzamide and[1,2,4]triazolo[1,5-a]pyridin-7-ylmethanamine forimidazo[1,2-a]pyridin-6-amine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.68 (s,1H), 8.89 (d, J=7.0 Hz, 1H), 8.64 (s, 1H), 8.45 (s, 1H), 7.65 (s, 1H),7.47-7.41 (m, 2H), 7.34-7.28 (m, 2H), 7.14 (dd, J=7.0, 1.8 Hz, 1H), 6.78(t, J=6.0 Hz, 1H), 4.42 (d, J=6.0 Hz, 2H), 2.29-2.15 (m, 3H), 1.79-1.68(m, 2H), 1.66-1.43 (m, 4H), 1.24-1.11 (m, 2H); MS (ESI(+)) m/e 393(M+H)⁺.

Example 565 tert-butyl4-(4-{[([1,2,4]triazolo[1,5-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide and[1,2,4]triazolo[1,5-a]pyridin-7-ylmethanamine forimidazo[1,2-a]pyridin-6-amine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.89 (d,J=7.0 Hz, 1H), 8.66 (s, 1H), 8.45 (s, 1H), 7.64 (s, 1H), 7.36-7.30 (m,2H), 7.14 (dd, J=7.0, 1.8 Hz, 1H), 7.12-7.07 (m, 2H), 6.80 (t, J=6.0 Hz,1H), 4.43 (d, J=6.0 Hz, 2H), 4.10-4.00 (m, 2H), 2.90-2.63 (m, 2H),2.66-2.54 (m, 1H), 1.75-1.67 (m, 2H), 1.49-1.35 (s, 11H); MS (ESI(+))m/e 451 (M+H)⁺.

Example 566N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-1-ylcarbonyl)benzamide

The title compound was prepared as described in Example 1A, substitutingpiperidine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.18 (t, J=5.9 Hz,1H), 8.49 (d, J=7.0 Hz, 1H), 7.96 (m, 2H), 7.89 (s, 1H), 7.52 (d, J=1.2Hz, 1H), 7.47 (m, 2H), 7.40 (s, 1H), 6.86 (dd, J=7.0, 1.7 Hz, 1H), 4.52(d, J=5.9 Hz, 2H), 3.59 (m, 2H), 3.24 (m, 2H), 1.66-1.38 (m, 6H); MS(ESI(+)) m/e 363 (M+H)⁺.

Example 5674-[1-(ethylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 557C,substituting ethane sulfonyl chloride for propane-2-sulfonyl chloride.¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.10 (t, J=6.0 Hz, 1H), 8.49 (dd, J=6.9,0.9 Hz, 1H), 7.93 (m, 2H), 7.88 (m, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.49(m, 2H), 7.39 (s, 1H), 6.86 (dd, J=7.0, 1.6 Hz, 1H), 4.51 (d, J=5.9 Hz,2H), 4.23 (m, 2H), 3.95 (m, 3H), 3.19 (q, J=7.3 Hz, 2H), 1.25 (t, J=7.3Hz, 3H); MS (ESI(+)) m/e 399 (M+H)⁺.

Example 5684-[1-(cyclopropylsulfonyl)azetidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 557C,substituting cyclopropane sulfonyl chloride for propane-2-sulfonylchloride. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.10 (t, J=6.0 Hz, 1H), 8.49(dd, J=6.9, 0.9 Hz, 1H), 7.93 (m, 2H), 7.88 (m, 1H), 7.52 (d, J=1.1 Hz,1H), 7.50 (m, 2H), 7.39 (s, 1H), 6.86 (dd, J=7.0, 1.6 Hz, 1H), 4.51 (d,J=5.9 Hz, 2H), 4.26 (t, J=7.7 Hz, 2H), 3.99 (m, 3H), 2.85 (m, 1H), 1.06(m, 2H), 0.97 (m, 2H); MS (ESI(+)) m/e 411 (M+H)⁺.

Example 569N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)azetidin-3-yl]benzamide

The title compound was prepared as described in Example 557C,substituting benzene sulfonyl chloride for propane-2-sulfonyl chloride.—¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.04 (t, J=5.9 Hz, 1H), 8.47 (m, 1H),7.92-7.82 (m, 4H), 7.75 (m, 4H), 7.51 (d, J=1.2 Hz, 1H), 7.36 (s, 1H),7.97 (m, 2H), 6.83 (dd, J=7.0, 1.6 Hz, 1H), 4.47 (d, J=5.9 Hz, 2H), 4.16(m, 2H), 3.79 (m, 1H), 3.67 (m, 2H); MS (ESI(+)) m/e 447 (M+H)⁺.

Example 570 propan-2-yl4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate

To a suspensionN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamide(0.103 g, 0.249 mmol) in dichloromethane (2 ml) was addedN-methylmorpholine (0.110 ml, 0.997 mmol) followed byisopropylchloroformate (0.374 ml, 0.374 mmol). A second portion ofisopropylchloroformate (0.4 ml) was added and after 1 hour the mixturewas directly purified by normal phase chromatography to give the titlecompound. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.05 (t, J=6.0 Hz, 1H), 8.51(d, J=7.0 Hz, 1H), 7.92 (s, 1H), 7.68 (d, J=3.8 Hz, 1H), 7.56 (d, J=1.2Hz, 1H), 7.40 (d, J=1.4 Hz, 1H), 6.96 (d, J=3.8 Hz, 1H), 6.88 (dd,J=7.0, 1.7 Hz, 1H), 4.78 (hept, J=6.2 Hz, 1H), 4.47 (d, J=5.9 Hz, 2H),4.05 (d, J=12.9 Hz, 2H), 3.10-2.97 (m, 1H), 2.98-2.81 (m, 2H), 2.01-1.88(m, 2H), 1.57-1.38 (m, 2H), 1.19 (d, J=6.2 Hz, 6H); MS (ESI(+)) m/e 427(M+H)⁺.

Example 571 2-methylpropyl4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}piperidine-1-carboxylate

The title compound was prepared as described in Example 570,substituting isobutyl carbonochloridate for isopropyl carbonochloridate.¹H NMR (300 MHz, DMSO-d₆) δ 8.99 (t, J=6.0 Hz, 1H), 8.48 (dd, J=7.0, 0.9Hz, 1H), 7.88 (t, J=1.0 Hz, 1H), 7.67 (d, J=3.9 Hz, 1H), 7.51 (d, J=1.1Hz, 1H), 7.37 (s, 1H), 6.96 (d, J=3.1 Hz, 1H), 6.82 (dd, J=7.0, 1.8 Hz,1H), 4.46 (d, J=5.8 Hz, 2H), 4.06 (d, J=13.3 Hz, 2H), 3.79 (d, J=6.6 Hz,2H), 3.13-2.97 (m, 1H), 2.97-2.80 (m, 2H), 2.03-1.77 (m, 3H), 1.48 (qd,J=12.5, 4.2 Hz, 2H), 0.89 (d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 441 (M+H)⁺.

Example 572N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 3,3,3-trifluoropropanoyl chloride for 2-cyclopentylacetylchloride andN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.00 (t,J=6.0 Hz, 1H), 8.48 (dd, J=6.9, 1.0 Hz, 1H), 7.88 (t, J=1.0 Hz, 1H),7.67 (d, J=3.8 Hz, 1H), 7.51 (d, J=1.3 Hz, 1H), 7.40-7.33 (m, 1H), 6.96(dd, J=3.7, 0.8 Hz, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 4.46 (d, J=6.3Hz, 2H), 3.90 (d, J=13.8 Hz, 1H), 3.66 (q, J=11.0 Hz, 2H), 3.23-3.04 (m,2H), 2.71 (td, J=12.8, 2.6 Hz, 1H), 2.07-1.88 (m, 2H), 1.71-1.31 (m,2H); MS (ESI(+)) m/e 451 (M+H)⁺.

Example 573N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]piperidin-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2-methylpropane-1-sulfonyl chloride for 2-cyclopentylacetylchloride andN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t,J=6.0 Hz, 1H), 8.48 (d, J=6.9 Hz, 1H), 7.89 (s, 1H), 7.68 (d, J=3.8 Hz,1H), 7.52 (d, J=1.1 Hz, 1H), 7.38 (s, 1H), 6.98 (d, J=3.8 Hz, 1H), 6.83(dd, J=7.0, 1.7 Hz, 1H), 4.46 (d, J=6.0 Hz, 2H), 3.71-3.59 (m, 2H), 2.99(tt, J=11.6, 3.6 Hz, 1H), 2.94-2.82 (m, 4H), 2.20-2.08 (m, 1H),2.08-1.97 (m, 2H), 1.62 (qd, J=12.6, 4.1 Hz, 2H), 1.04 (d, J=6.7 Hz,6H); MS (ESI(+)) m/e 461 (M+H)⁺.

Example 574N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 4,4,4-trifluorobutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00 (t, J=6.0 Hz,1H), 8.48 (d, J=6.8 Hz, 1H), 7.89 (s, 1H), 7.68 (d, J=3.8 Hz, 1H), 7.52(d, J=1.2 Hz, 1H), 7.41-7.34 (m, 1H), 6.96 (d, J=3.8 Hz, 1H), 6.83 (dd,J=7.0, 1.7 Hz, 1H), 4.54-4.38 (m, 3H), 4.02-3.88 (m, 1H), 3.12 (tdt,J=11.3, 7.9, 3.1 Hz, 2H), 2.76-2.41 (m, 5H), 2.06-1.88 (m, 2H), 1.58(qd, J=12.3, 4.0 Hz, 1H), 1.42 (qd, J=12.5, 4.2 Hz, 1H); MS (ESI(+)) m/e465 (M+H)⁺.

Example 575N-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide

A solution ofN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(1-isobutyrylpiperidin-4-yl)benzamide(0.025 g, 0.062 mmol) in chloroform (1.030 ml) was treated withN-chlorosuccinimide (9.49 mg, 0.071 mmol) and the reaction was stirredat ambient temperature for 16 hours. The reaction was concentrated undera stream of warm nitrogen. The residue was purified by normal phasechromatography to give the title compound. ¹H NMR (500 MHz, methanol-d₄)δ ppm 8.67 (d, J=7.0 Hz, 1H), 8.11 (s, 1H), 7.89-7.83 (m, 2H), 7.81 (s,1H), 7.57 (dd, J=7.1, 1.5 Hz, 1H), 7.43-7.37 (m, 2H), 4.80-4.75 (m, 2H),4.75-4.67 (m, 1H), 4.25-4.16 (m, 1H), 3.28-3.18 (m, 1H), 3.07-2.88 (m,2H), 2.79-2.66 (m, 1H), 2.02-1.85 (m, 2H), 1.75-1.53 (m, 2H), 1.17-1.08(m, 6H); MS (ESI(+)) m/e 439 (M+H)⁺.

Example 576N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-methyltetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.02 (t, J=6.0 Hz,1H), 8.49 (dd, J=7.1, 1.0 Hz, 1H), 8.13 (s, 1H), 7.89 (t, J=1.0 Hz, 1H),7.81 (s, 1H), 7.74 (d, J=3.8 Hz, 1H), 7.52 (d, J=1.3 Hz, 1H), 7.43-7.36(m, 1H), 7.23 (d, J=3.8 Hz, 1H), 6.85 (dd, J=7.1, 1.7 Hz, 1H), 4.48 (d,J=5.9 Hz, 2H), 4.04 (s, 2H), 3.68 (dt, J=11.8, 4.6 Hz, 2H), 3.52 (ddd,J=11.9, 9.1, 3.0 Hz, 2H), 1.51 (ddd, J=13.4, 9.2, 4.2 Hz, 2H), 1.24 (dt,J=13.4, 4.0 Hz, 2H), 0.96 (s, 3H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 5775-[1-(2-cyano-2-methylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting2,2-dimethyl-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)propanenitrileand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ 9.05 (t, J=6.0 Hz, 1H),8.49 (dd, J=6.8, 1.0 Hz, 1H), 8.19 (d, J=0.7 Hz, 1H), 7.92 (s, 1H),7.90-7.88 (m, 1H), 7.76 (d, J=3.8 Hz, 1H), 7.52 (d, J=1.1 Hz, 1H),7.43-7.36 (m, 1H), 7.27 (d, J=3.8 Hz, 1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H),4.48 (d, J=5.7 Hz, 2H), 4.35 (s, 2H), 1.35 (s, 6H); MS (ESI(+)) m/e 405(M+H)⁺.

Example 578

4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

Example 578A 1-(5-bromo-4-chlorothiophen-2-yl)ethanone

2-Bromo-3-chlorothiophene (10.7 g, 51.5 mmol) was dissolved indichloromethane (73.5 ml). The flask was equipped with a desiccantfilled drying tube and the solution was chilled in an ice bath. Acetylchloride (6.06 g, 77 mmol) was added followed by addition of aluminumtrichloride (8.24 g, 61.8 mmol) over about 2 minutes (reaction bubbledvigorously as aluminum trichloride was added). The reaction mixture wasstirred overnight, allowing to warm to room temperature, and then addedcautiously and with stirring to a 1-L beaker containing ˜200 mL satsodium bicarbonate. The mixture was stirred for 30 minutes and dilutedwith dichloromethane (A100 mL). The layers were separated and theorganic layer was washed with aqueous saturated sodium bicarbonate,water, and brine. The combined organic layers were dried with sodiumsulfate, filtered, and concentrated to give a crude solid. This materialwas recrystallized from hot hexanes to give the title compound.

Example 578B 5-bromo-4-chlorothiophene-2-carboxylic acid

Sodium hydroxide (50% in water) (5.82 ml, 110 mmol) was added to water(15 ml), and the mixture was chilled to 0° C. Bromine solution (1.669ml, 32.6 mmol) was added, followed by dropwise addition of a solution of1-(5-bromo-4-chlorothiophen-2-yl)ethanone (2.4 g, 10.02 mmol) in dioxane(18 ml). The mixture was stirred for 1.5 hours at room temperature,washed with dichloromethane, and then the aqueous phase was adjusted topH 1 using 4N aqueous HCl. The precipitated solid was collected byfiltration to give the title compound.

Example 578C4-chloro-5-(1-isobutyl-1H-pyrazol-4-yl)thiophene-2-carboxylic acid

The title compound was prepared as described in Example 51A,substituting 5-bromo-4-chlorothiophene-2-carboxylic acid for4-bromoaniline.

Example 578D4-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-chloro-5-(1-isobutyl-1H-pyrazol-4-yl)thiophene-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.17 (t, J=5.9 Hz,1H), 8.50 (d, J=7.0 Hz, 1H), 8.31 (s, 1H), 7.93-7.88 (m, 2H), 7.83 (s,1H), 7.53 (d, J=1.1 Hz, 1H), 7.42 (s, 1H), 6.85 (dd, J=7.0, 1.6 Hz, 1H),4.49 (d, J=5.9 Hz, 2H), 3.98 (d, J=7.2 Hz, 2H), 2.20-2.08 (m, 1H), 0.86(d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 414 (M+H)⁺.

Example 5794-chloro-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(3R)-tetrahydrofuran-3-ylmethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and(R)-4-chloro-5-(1-((tetrahydrofuran-3-yl)methyl)-1H-pyrazol-4-yl)thiophene-2-carboxylicacid for 4-nitrobenzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.17 (t,J=6.0 Hz, 1H), 8.50 (d, J=7.0 Hz, 1H), 8.28 (s, 1H), 7.93-7.88 (m, 2H),7.83 (s, 1H), 7.53 (d, J=1.2 Hz, 1H), 7.42 (s, 1H), 6.85 (dd, J=7.0, 1.7Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.28-4.15 (m, 3H), 3.78-3.72 (m, 1H),3.67-3.61 (m, 1H), 1.98-1.90 (m, 1H), 1.84-1.70 (m, 2H), 1.65-1.57 (m,1H); MS (ESI(+)) m/e 442 (M+H)⁺.

Example 6215-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamideExample 621AN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromothiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amineand 5-bromothiophene-2-carboxylic acid for 4-nitrobenzoic acid.

Example 621B5-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting2-methyl-1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)propan-2-olfor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromothiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=5.9 Hz,1H), 8.88 (s, 1H), 8.48 (s, 1H), 8.04 (d, J=0.5 Hz, 1H), 7.84 (dd,J=9.2, 0.7 Hz, 1H), 7.79 (d, J=0.5 Hz, 1H), 7.71 (d, J=3.9 Hz, 1H), 7.66(dd, J=9.2, 1.7 Hz, 1H), 7.22 (d, J=3.9 Hz, 1H), 4.72 (s, 1H), 4.54 (d,J=5.8 Hz, 2H), 4.03 (s, 2H), 1.08 (s, 6H); MS (ESI(+)) m/e 397 (M+H)⁺.

Example 6225-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-methyltetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromothiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=5.9 Hz,1H), 8.88 (s, 1H), 8.48 (s, 1H), 8.04 (d, J=0.5 Hz, 1H), 7.84 (dd,J=9.2, 0.7 Hz, 1H), 7.79 (d, J=0.5 Hz, 1H), 7.71 (d, J=3.9 Hz, 1H), 7.66(dd, J=9.2, 1.7 Hz, 1H), 7.22 (d, J=3.9 Hz, 1H), 4.72 (s, 1H), 4.54 (d,J=5.8 Hz, 2H), 4.03 (s, 2H), 1.08 (s, 6H); MS (ESI(+)) m/e 437 (M+H)⁺.

Example 623N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)azetidin-3-yl]benzamide

The title compound was prepared as described in Example 557C,substituting methane sulfonyl chloride for propane-2-sulfonyl chloride.¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.11 (t, J=6.0 Hz, 1H), 8.49 (m, 1H),7.91 (m, 2H), 7.88 (m, 1H), 7.52 (m, 2H), 7.49 (m, 1H), 7.39 (s, 1H),6.86 (dd, J=7.0, 1.7 Hz, 1H), 4.51 (d, J=5.9 Hz, 2H), 4.23 (m, 2H), 3.95(m, 3H), 3.08 (s, 3H); MS (ESI(+)) m/e 385 (M+H)⁺.

Example 624N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(methylsulfonyl)pyrrolidin-3-yl]benzamide

The title compound was prepared as described in Example 557C,substituting methane sulfonyl chloride for propane-2-sulfonyl chlorideand N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamidefor 4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide. HNMR (400 MHz, DMSO-d₆) δ ppm 9.07 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9,0.9 Hz, 1H), 7.88 (m, 3H), 7.52 (d, J=1.2 Hz, 1H), 7.45 (m, 2H), 7.38(m, 1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 4.51 (d, J=5.9 Hz, 2H), 3.73 (dd,J=9.6, 7.5 Hz, 1H), 3.47 (m, 2H), 3.35 (m, 1H), 3.19 (t, J=9.6 Hz, 1H),2.97 (s, 3H), 2.31 (m, 1H), 2.02 (m, 1H); MS (ESI(+)) m/e 399 (M+H)⁺.

Example 6254-[1-(ethylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 557C,substituting ethane sulfonyl chloride for propane-2-sulfonyl chlorideand N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamidefor 4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide. HNMR (400 MHz, DMSO-d₆) δ ppm 9.07 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9,0.9 Hz, 1H), 7.88 (m, 3H), 7.52 (d, J=1.2 Hz, 1H), 7.45 (m, 2H), 7.38(s, 1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 4.50 (d, J=5.9 Hz, 2H), 3.75 (dd,J=9.5, 7.5 Hz, 1H), 3.50 (m, 2H), 3.38 (m, 1H), 3.26-3.12 (m, 3H), 2.32(m, 1H), 2.03 (m, 1H), 1.24 (t, J=7.3 Hz, 3H); MS (ESI(+)) m/e 413(M+H)⁺.

Example 6264-[1-(cyclopropylsulfonyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 557C,substituting cyclopropane sulfonyl chloride for propane-2-sulfonylchloride andN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamide for4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 9.07 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9, 0.9Hz, 1H), 7.88 (m, 3H), 7.51 (d, J=1.2 Hz, 1H), 7.45 (m, 2H), 7.38 (m,1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 4.50 (d, J=5.9 Hz, 2H), 3.79 (dd,J=9.7, 7.5 Hz, 1H), 3.53 (m, 2H), 3.43 (m, 1H), 3.23 (m, 1H), 2.78 (m,1H), 2.34 (m, 1H), 2.01 (m, 1H), 0.98 (m, 4H); MS (ESI(+)) m/e 425(M+H)⁺.

Example 627N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)pyrrolidin-3-yl]benzamide

The title compound was prepared as described in Example 557C,substituting benzene sulfonyl chloride for propane-2-sulfonyl chlorideand N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamidefor 4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.04 (t, J=5.9 Hz, 1H), 8.48 (dd, J=6.9,0.9 Hz, 1H), 7.87 (m, 3H), 7.81 (m, 2H), 7.74 (m, 1H), 7.66 (m, 2H),7.51 (d, J=1.2 Hz, 1H), 7.37 (m, 1H), 7.25 (m, 2H), 6.84 (dd, J=6.9, 1.7Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 3.72 (dd, J=9.8, 7.5 Hz, 1H), 3.46 (m,1H), 3.26 (m, 2H), 3.11 (m, 1H), 2.17 (m, 1H), 1.78 (m, 1H); MS (ESI(+))m/e 461 (M+H)⁺.

Example 672N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)pyrrolidin-3-yl]benzamide

The title compound was prepared as described in Example 557C,substituting propane-2-sulfonyl chloride for propane-2-sulfonyl chlorideand N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(pyrrolidin-3-yl)benzamidefor 4-(azetidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide. ¹HNMR (501 MHz, DMSO-d₆) δ ppm 9.04 (t, J=6.0 Hz, 1H), 8.47 (d, J=6.9 Hz,1H), 7.87 (m, 3H), 7.50 (d, J=1.2 Hz, 1H), 7.43 (m, 2H), 7.37 (s, 1H),6.84 (dd, J=7.0, 1.6 Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 3.77 (m, 1H), 3.52(m, 2H), 3.42 (m, 2H), 3.25 (m, 1H), 2.30 (m, 1H), 2.04 (m, 1H), 1.25(dd, J=6.8, 1.4 Hz, 6H); MS (ESI(+)) m/e 427 (M+H)⁺.

Example 6731-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(2-methoxyethyl)-1H-pyrazol-4-yl]phenyl}urea

The title compound was prepared as described in Example 51A,substituting1-(2-methoxyethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea for4-bromoaniline. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.66 (s, 1H), 8.50 (d,J=7.0 Hz, 1H), 8.01 (s, 1H), 7.90 (s, 1H), 7.77 (s, 1H), 7.54 (s, 1H),7.40 (m, 5H), 6.87 (dd, J=7.0, 1.6 Hz, 1H), 6.71 (t, J=6.0 Hz, 1H), 4.34(d, J=6.0 Hz, 2H), 4.23 (t, J=5.3 Hz, 2H), 3.69 (t, J=5.3 Hz, 2H), 3.23(s, 3H); MS (ESI(+)) m/e 391 (M+H)⁺.

Example 6741-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydrofuran-2-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea

The title compound was prepared as described in Example 51A,substituting1-(tetrahydrofuran-2-ylmethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea for4-bromoaniline. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.64 (s, 1H), 8.47 (d,J=7.0 Hz, 1H), 8.00 (s, 1H), 7.87 (s, 1H), 7.77 (s, 1H), 7.50 (d, J=1.2Hz, 1H), 7.40 (m, 5H), 6.83 (dd, J=7.0, 1.6 Hz, 1H), 6.70 (t, J=6.0 Hz,1H), 4.33 (d, J=6.0 Hz, 2H), 4.13 (m, 3H), 3.74 (m, 1H), 3.62 (m, 1H),1.91 (m, 1H), 1.76 (m, 2H), 1.60 (m, 1H); MS (ESI(+)) m/e 417 (M+H)⁺.

Example 6751-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1H-pyrazol-4-yl]phenyl}urea

The title compound was prepared as described in Example 51A,substituting1-(tetrahydro-2H-pyran-4-ylmethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 1-(4-bromophenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea for4-bromoaniline. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.64 (s, 1H), 8.47 (d,J=7.0 Hz, 1H), 8.02 (s, 1H), 7.87 (s, 1H), 7.77 (d, J=0.8 Hz, 1H), 7.50(d, J=1.2 Hz, 1H), 7.40 (m, 5H), 6.83 (dd, J=7.0, 1.6 Hz, 1H), 6.70 (t,J=6.0 Hz, 1H), 4.32 (d, J=5.9 Hz, 2H), 3.98 (d, J=7.1 Hz, 2H), 3.81 (m,2H), 3.23 (m, 2H), 2.05 (m, 1H), 1.40 (m, 2H), 1.23 (m, 2H); MS (ESI(+))m/e 431 (M+H)⁺.

Example 6765-[1-(1,4-dioxan-2-ylmethyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((1,4-dioxan-2-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromothiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=5.9 Hz,1H), 8.90-8.85 (m, 1H), 8.48 (s, 1H), 8.12 (s, 1H), 7.84 (dd, J=9.2, 0.8Hz, 1H), 7.82 (d, J=0.6 Hz, 1H), 7.71 (d, J=3.9 Hz, 1H), 7.66 (dd,J=9.2, 1.7 Hz, 1H), 7.22 (d, J=3.9 Hz, 1H), 4.54 (d, J=5.8 Hz, 2H),4.20-4.12 (m, 2H), 3.95-3.83 (m, 1H), 3.74 (dd, J=11.4, 2.5 Hz, 2H),3.68-3.60 (m, 1H), 3.59-3.39 (m, 2H), 3.29-3.21 (m, 1H); MS (ESI(+)) m/e425 (M+H)⁺.

Example 6775-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.00 (t,J=6.0 Hz, 1H), 8.48 (dd, J=7.0, 0.8 Hz, 1H), 7.91-7.85 (m, 1H), 7.67 (d,J=3.8 Hz, 1H), 7.55-7.35 (m, 4H), 7.34-7.25 (m, 2H), 6.98 (dd, J=3.8,0.5 Hz, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 4.60 (d, J=13.2 Hz, 1H), 4.46(d, J=5.9 Hz, 2H), 3.45 (d, J=12.7 Hz, 1H), 3.28-3.08 (m, 2H), 2.93 (td,J=12.8, 2.5 Hz, 1H), 2.00 (dd, J=43.2, 12.5 Hz, 2H), 1.68-1.39 (m, 2H);MS (ESI(+)) m/e 463 (M+H)⁺.

Example 678 tert-butyl4-{4-[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (500 MHz, methanol-d₄) δ ppm 9.00-8.96 (m, 1H), 8.51-8.46(m, 1H), 8.04-8.00 (m, 1H), 7.89-7.81 (m, 2H), 7.81-7.77 (m, 1H),7.39-7.32 (m, 2H), 4.68 (s, 2H), 4.27-4.16 (m, 2H), 2.97-2.70 (m, 3H),1.92-1.78 (m, 2H), 1.71-1.50 (m, 2H), 1.48 (s, 9H); MS (ESI(+)) m/e 436(M+H)⁺.

Example 6794-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(2-cyclopentylacetamido)benzoic acid for 4-nitrobenzoic acid. ¹H NMR(500 MHz, methanol-d₄) δ ppm 9.19 (d, J=0.9 Hz, 1H), 8.65 (d, J=1.2 Hz,1H), 8.20 (d, J=1.1 Hz, 1H), 8.03 (d, J=1.5 Hz, 1H), 7.90-7.83 (m, 2H),7.73-7.66 (m, 2H), 4.74 (s, 2H), 2.44-2.22 (m, 3H), 1.92-1.76 (m, 2H),1.76-1.49 (m, 4H), 1.35-1.14 (m, 2H); MS (ESI(+)) m/e 378 (M+H)⁺.

Example 680 tert-butyl4-(4-{[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyrazin-6-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (500 MHz, methanol-d₄) δ ppm8.99-8.95 (m, 1H), 8.48-8.44 (m, 1H), 8.02 (s, 1H), 7.81-7.77 (m, 1H),7.33-7.26 (m, 2H), 7.15-7.09 (m, 2H), 4.49 (s, 2H), 4.22-4.14 (m, 2H),2.92-2.73 (m, 2H), 2.74-2.58 (m, 1H), 1.82-1.74 (m, 2H), 1.61-1.41 (m,11H); MS (ESI(+)) m/e 451 (M+H)⁺.

Example 6812-cyclopentyl-N-(4-{[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]amino}phenyl)acetamide

The title compound was prepared as described in Example 1C, substitutingN-(4-aminophenyl)-2-cyclopentylacetamide for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyrazin-6-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (500 MHz, methanol-d₄) δ ppm9.17-9.13 (m, 1H), 8.60 (s, 1H), 8.18 (s, 1H), 7.99 (d, J=1.5 Hz, 1H),7.46-7.40 (m, 2H), 7.35-7.29 (m, 2H), 4.56 (bs, 2H), 2.37-2.23 (m, 3H),1.90-1.77 (m, 2H), 1.77-1.49 (m, 4H), 1.34-1.17 (m, 2H); MS (ESI(+)) m/e393 (M+H)⁺.

Example 682N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide

A solution ofN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide (0.05g, 0.150 mmol) in tetrahydrofuran (1.246 ml) was treated with sodiumhydride (0.018 g, 0.449 mmol) in 3 portions. The reaction was stirred atambient temperature for 45 minutes and became a partially homogeneoussolution. Benzenesulfonyl chloride (0.021 ml, 0.164 mmol) was added andthe mixture was stirred for 16 hours. The reaction was treated with 0.1mL water and was concentrated under a stream of nitrogen. Reverse-phasechromatography provided the title compound. ¹H NMR (500 MHz,methanol-d₄) δ ppm 8.73 (dd, J=7.0, 0.9 Hz, 1H), 8.15 (dd, J=2.2, 0.8Hz, 1H), 7.97 (d, J=2.2 Hz, 1H), 7.89-7.75 (m, 5H), 7.73-7.59 (m, 3H),7.46 (dd, J=7.0, 1.6 Hz, 1H), 7.37-7.31 (m, 2H), 4.75 (s, 2H), 3.96-3.88(m, 2H), 2.67-2.52 (m, 1H), 2.48-2.37 (m, 2H), 1.95-1.72 (m, 4H); MS(ESI(+)) m/e 475 (M+H)⁺.

Example 683N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 682,substituting propane-2-sulfonyl chloride for benzenesulfonyl chloride.¹H NMR (500 MHz, methanol-d₄) δ ppm 8.75 (d, J=7.0 Hz, 1H), 8.17 (d,J=2.2 Hz, 1H), 7.99 (d, J=2.2 Hz, 1H), 7.89-7.83 (m, 2H), 7.80 (s, 1H),7.49 (dd, J=7.0, 1.6 Hz, 1H), 7.43-7.37 (m, 2H), 4.77 (s, 2H), 3.95-3.87(m, 2H), 3.38-3.29 (m, 1H), 3.12-3.00 (m, 2H), 2.89-2.75 (m, 1H),1.95-1.86 (m, 2H), 1.82-1.68 (m, 2H), 1.34 (d, J=6.8 Hz, 6H); MS(ESI(+)) m/e 417 (M+H)⁺.

Example 6844-[1-(cyclopropylsulfonyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide

The title compound was prepared as described in Example 682,substituting cyclopropanesulfonyl chloride for benzenesulfonyl chloride.¹H NMR (500 MHz, methanol-d₄) δ ppm 8.75 (dd, J=7.0, 0.9 Hz, 1H),8.19-8.15 (m, 1H), 7.98 (d, J=2.2 Hz, 1H), 7.90-7.84 (m, 2H), 7.80 (s,1H), 7.48 (dd, J=7.0, 1.6 Hz, 1H), 7.45-7.38 (m, 2H), 4.77 (s, 2H),3.92-3.84 (m, 2H), 3.07-2.96 (m, 2H), 2.86-2.73 (m, 1H), 2.57-2.46 (m,1H), 2.00-1.91 (m, 2H), 1.88-1.73 (m, 2H), 1.13-0.99 (m, 4H); MS(ESI(+)) m/e 439 (M+H)⁺.

Example 6855-{(1R)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 685A tert-butyl 5-formylthiophene-2-carboxylate

5-Formylthiophene-2-carboxylic acid (5.3 g, 33.9 mmol) was taken up intetrahydrofuran (100 ml) and boc-anhydride (16.30 g, 74.7 mmol) wasadded, followed by N,N-dimethylaminopyridine (0.829 g, 6.79 mmol). Themixture was stirred overnight at room temperature, during which time thereaction became a dark, purplish color. It was diluted with sat sodiumbicarbonate and extracted with ether. The organic layers were driedsodium sulfate, concentrated then purified by normal phasechromatography to give the title compound.

Example 685B (S,E)-tert-butyl5-(((tert-butylsulfinyl)imino)methyl)thiophene-2-carboxylate

tert-Butyl 5-formylthiophene-2-carboxylate (2 g, 9.42 mmol) and(S)-2-methylpropane-2-sulfinamide (1.370 g, 11.31 mmol) were dissolvedin dichloromethane (100 ml). The mixture was chilled in an ice bath towhich was added tetraethoxytitanium (8.7 ml, 41.5 mmol). The mixture wasallowed to warm to room temperature overnight with stirring.

The mixture was poured into a large Erlenmeyer flask with 200 mLdichloromethane and was diluted with 18 mL H₂O. After vigorous stirringfor 30 minutes the suspension was filtered through diatomaceous earthand the filtrate was concentrated. Purification using normal phasechromatography provided the title compound.

Example 685C tert-butyl5-((R)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylateand tert-butyl5-((S)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylate

(S,E)-tert-Butyl5-((tert-butylsulfinylimino)methyl)thiophene-2-carboxylate (1 g, 3.17mmol) was dissolved in dichloromethane (15.85 ml) and chilled to −45° C.in an acetone bath to which dry ice had been added to achieve thedesired temperature. Isobutylmagnesium bromide (2.0M in diethyl ether;3.17 ml, 6.34 mmol) was added dropwise over −5 minutes. The mixture wasstirred for 4 hours keeping the temperature between −40° C. and −50° C.by periodic addition of dry ice and then warmed to room temperatureovernight. The mixture was quenched with saturated ammonium chloride(exothermic, bubbling) and extracted with dichloromethane (three times;considerable emulsion formed). The organic extracts were dried withsodium sulfate, filtered, concentrated and chromatographed to provideboth tert-butyl5-((R)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylateand tert-butyl5-((S)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylateas separate compounds.

Example 685D (R)-tert-butyl5-(1-amino-3-methylbutyl)thiophene-2-carboxylate

The title compound was prepared as described in Example 324C,substituting tert-butyl5-((R)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylatefor tert-butyl5-((R)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylate.

Example 685E(R)-5-(1-(cyclopropanecarboxamido)-3-methylbutyl)thiophene-2-carboxylicacid

The title compound was prepared as described in Example 1A, substituting(R)-tert-butyl 5-(1-amino-3-methylbutyl)thiophene-2-carboxylate for3-methylbutan-1-amine and cyclopropanecarboxylic acid for 4-nitrobenzoicacid followed by acidic deprotection as described in Example 28A,substituting (R)-tert-butyl5-(1-(cyclopropanecarboxamido)-3-methylbutyl)thiophene-2-carboxylate fortert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 685F5-{(1R)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and(R)-5-(1-(cyclopropanecarboxamido)-3-methylbutyl)thiophene-2-carboxylicacid for 4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.00 (t,J=6.0 Hz, 1H), 8.55 (d, J=8.4 Hz, 1H), 8.48 (d, J=7.4 Hz, 1H), 7.88 (d,J=1.1 Hz, 1H), 7.64 (d, J=3.8 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.37 (s,1H), 6.98 (d, J=3.8 Hz, 1H), 6.82 (dd, J=7.0, 1.7 Hz, 1H), 5.11 (td,J=8.8, 5.0 Hz, 1H), 4.46 (d, J=5.9 Hz, 2H), 1.80-1.52 (m, 4H), 0.95-0.83(m, 6H), 0.75-0.59 (m, 4H); MS (ESI(+)) m/e 411 (M+H)⁺.

Example 686N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{(1R)-3-methyl-1-[(tetrahydrofuran-3-ylacetyl)amino]butyl}thiophene-2-carboxamide

The title compound was described as in Example 685, substituting2-(tetrahydrofuran-3-yl)acetic acid for cyclopropanecarboxylic acid inExample 685E. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.00 (t, J=6.0 Hz, 1H),8.48 (d, J=7.0 Hz, 1H), 8.39 (d, J=8.5 Hz, 1H), 7.88 (s, 1H), 7.64 (d,J=3.7 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.37 (s, 1H), 6.97 (d, J=3.8 Hz,1H), 6.82 (dd, J=7.0, 1.7 Hz, 1H), 5.16-5.05 (m, 1H), 4.45 (d, J=5.9 Hz,2H), 3.76-3.51 (m, 3H), 3.29-3.21 (m, 1H), 2.29-2.16 (m, 3H), 2.02-1.86(m, 1H), 1.78-1.40 (m, 4H), 0.99-0.77 (m, 6H); MS (ESI(+)) m/e 455(M+H)⁺.

Example 6875-{(1S)-1-[(cyclopropylcarbonyl)amino]-3-methylbutyl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was described as in Example 685, substituting butyl5-((S)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylatefor tert-butyl5-((R)-1-((S)-1,1-dimethylethylsulfinamido)-3-methylbutyl)thiophene-2-carboxylatein Example 685D. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04-8.96 (m, 1H), 8.55(d, J=8.4 Hz, 1H), 8.48 (dd, J=7.0, 0.9 Hz, 1H), 7.88 (s, 1H), 7.64 (d,J=3.8 Hz, 1H), 7.52 (d, J=1.1 Hz, 1H), 7.37 (s, 1H), 6.98 (d, J=3.8 Hz,1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 5.17-5.05 (m, 1H), 4.46 (d, J=5.9 Hz,2H), 1.77-1.44 (m, 4H), 1.01-0.77 (m, 6H), 0.66 (d, J=7.2 Hz, 4H); MS(ESI(+)) m/e 411 (M+H)⁺.

Example 688N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1-phenylpiperidin-4-yl)-1,3-thiazole-5-carboxamideExample 688A ethyl 2-(piperidin-4-yl)thiazole-5-carboxylate

Ethyl 3-ethoxyacrylate (1.50 g, 10.38 mml) was dissolved indioxane/water and chilled to −10° C. N-Bromosuccinimide (2.03 g, 11.42mmol) was added and the mixture was stirred 1 hour at room temperature.tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (2.54 g, 10.38 mmol)was added and the mixture was heated at 100° C. for 1 hour. The reactionmixture was poured into 25 mL saturated ammonium hydroxide and extractedwith dichloromethane. The combined organic layers were washed withbrine, dried with sodium sulfate, filtered, and concentrated. Normalphase chromatography provided the title compound.

Example 688B ethyl 2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate

Ethyl 2-(piperidin-4-yl)thiazole-5-carboxylate (100 mg, 0.416 mmol),2,2′-bis(diphenylphosphino)-1,1′-binaphthalene (21 mg, 0.033 mmol),bis(dibenzylideneacetone)palladium(0) (15 mg, 0.017 mmol) and cesiumcarbonate (678 mg, 2.081 mmol) were placed in a pressure tube cappedwith a septum and degassed with nitrogen by passing a stream through thevessel for 30 minutes. Separately, bromobenzene (68.6 mg, 0.437 mmol)was dissolved in toluene (2 ml) and the solution was degassed bybubbling nitrogen for 30 minutes. The bromobenzene solution was added tothe solid mixture and the sealed tube was heated to 100° C. overnight.The mixture was partitioned between dichloromathane and water and thecombined organic layers were concentrated and purified by normal phasechromatography to give the title compound.

Example 688C lithium 2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate

A solution of ethyl 2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate (31mg, 0.098 mmol) in 1 ml of 1:1 tetrahydrofuran/methanol was treated with1M aqueous LiOH (0.11 ml, 0.11 mol) and stirred at 65° C. for 3 hours.The mixture was taken to dryness and used directly in the next step.

Example 688DN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(1-phenylpiperidin-4-yl)-1,3-thiazole-5-carboxamide

Lithium 2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate (28.8 mg, 0.098mmol), imidazo[1,2-a]pyridin-7-ylmethanamine (17.31 mg, 0.118 mmol),4-methylmorpholine (49.6 mg, 0.490 mmol) and2-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)-1,1,3,3-tetramethylisouroniumhexafluorophosphate(V) (55.9 mg, 0.147 mmol) were combined in a vialwith dichloromethane (2.5 ml) and the reaction was stirred overnight.The mixture was partitioned between dichloromethane and saturated sodiumbicarbonate. The organic layers were dried with sodium sulfate,filtered, and concentrated. Trituration of the crude material withdichloromethane provided the title compound. ¹H NMR (300 MHz, DMSO-d₆) δppm 9.21 (t, J=5.9 Hz, 1H), 8.49 (dd, J=7.0, 0.9 Hz, 1H), 8.34 (s, 1H),7.91-7.88 (m, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.43-7.38 (m, 1H), 7.26-7.16(m, 2H), 7.01-6.93 (m, 2H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 6.81-6.72 (m,1H), 4.48 (d, J=5.9 Hz, 2H), 3.81-3.73 (m, 2H), 3.24-3.01 (m, 1H),2.90-2.78 (m, 2H), 2.19-2.09 (m, 2H), 1.90-1.73 (m, 2H); MS (ESI(+)) m/e418 (M+H)⁺.

Example 697N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(pyridin-2-yl)piperidin-4-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 688,substituting 2-bromopyridine for bromobenzene in Example 688B. ¹H NMR(400 MHz, DMSO-d₆) δ ppm 9.21 (t, J=5.9 Hz, 1H), 8.49 (dd, J=6.9, 0.9Hz, 1H), 8.33 (s, 1H), 8.13-8.09 (m, 1H), 7.89 (s, 1H), 7.55-7.48 (m,2H), 7.40 (s, 1H), 6.86 (d, J=8.7 Hz, 1H), 6.83 (dd, J=7.0, 1.6 Hz, 1H),6.61 (dd, J=6.9, 5.1 Hz, 1H), 4.48 (d, J=5.9 Hz, 2H), 4.40-4.32 (m, 2H),3.03-2.92 (m, 2H), 2.14-2.05 (m, 2H), 1.68 (qd, J=12.5, 3.9 Hz, 2H); MS(ESI(+)) m/e 419 (M+H)⁺.

Example 6985-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-fluorotetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=6.0 Hz,1H), 8.49 (d, J=7.1 Hz, 1H), 8.11 (s, 1H), 7.89 (s, 1H), 7.85 (s, 1H),7.75 (d, J=3.9 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.40 (s, 1H), 7.26 (d,J=3.9 Hz, 1H), 6.85 (dd, J=7.0, 1.6 Hz, 1H), 4.48 (d, J=5.9 Hz, 2H),4.42 (d, J=21.4 Hz, 2H), 3.74 (ddd, J=11.4, 4.6, 2.9 Hz, 2H), 3.51 (td,J=11.3, 2.0 Hz, 2H), 1.92-1.64 (m, 2H), 1.55 (t, J=11.8 Hz, 2H); MS(ESI(+)) m/e 440 (M+H)⁺.

Example 734N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamideExample 734A5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-bromofuran-2-carboxylic acid for 4-nitrobenzoic acid.

Example 734BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-methyltetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand bromide for 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.89 (t,J=6.1 Hz, 1H), 8.49 (dd, J=7.0, 0.9 Hz, 1H), 8.13 (d, J=0.5 Hz, 1H),7.91-7.86 (m, 2H), 7.52 (d, J=1.2 Hz, 1H), 7.40 (s, 1H), 7.17 (d, J=3.6Hz, 1H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 6.67 (d, J=3.5 Hz, 1H), 4.49 (d,J=6.0 Hz, 2H), 4.07 (s, 2H), 3.68 (dt, J=11.5, 4.5 Hz, 2H), 3.51 (ddd,J=11.9, 9.3, 3.0 Hz, 2H), 1.51 (ddd, J=13.4, 9.2, 4.2 Hz, 2H), 1.33-1.15(m, 2H), 0.96 (s, 3H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 7355-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamideExample 735A tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)furan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline.

Example 735B tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)furan-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1B, substitutingtert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)furan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor N-isopentyl-4-nitrobenzamide.

Example 735CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)furan-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)furan-2-yl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 735D5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.85 (t, J=6.1 Hz, 1H), 8.47 (dd,J=7.0, 0.8 Hz, 1H), 7.92-7.83 (m, 1H), 7.55-7.45 (m, 2H), 7.41 (td,J=7.5, 1.5 Hz, 1H), 7.37 (s, 1H), 7.34-7.25 (m, 2H), 7.06 (d, J=3.4 Hz,1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 6.33 (dd, J=3.5, 0.7 Hz, 1H), 4.53(d, J=13.4 Hz, 1H), 4.44 (d, J=6.0 Hz, 2H), 3.44 (d, J=13.0 Hz, 1H),3.19 (t, J=12.8 Hz, 1H), 3.11-2.90 (m, 2H), 2.09 (d, J=11.0 Hz, 1H),1.94 (d, J=11.9 Hz, 1H), 1.73-1.42 (m, 2H); MS (ESI(+)) m/e 447 (M+H)⁺.

Example 736N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(piperidin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.84 (t, J=6.1 Hz, 1H), 8.47 (dd, J=7.0,0.8 Hz, 1H), 7.94-7.82 (m, 1H), 7.51 (d, J=1.2 Hz, 1H), 7.42-7.33 (m,1H), 7.05 (d, J=3.4 Hz, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 6.31 (dd,J=3.4, 0.6 Hz, 1H), 4.44 (d, J=6.0 Hz, 3H), 4.06-3.90 (m, 1H), 3.21-3.07(m, 1H), 3.07-2.77 (m, 2H), 2.77-2.59 (m, 1H), 2.06-1.90 (m, 2H),1.61-1.37 (m, 2H), 0.99 (d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 395 (M+H)⁺.

Example 738N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1-(2,2,2-trifluoroethyl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.21 (t, J=5.9 Hz, 1H),8.49 (dd, J=6.9, 0.9 Hz, 1H), 8.33 (s, 1H), 8.13-8.09 (m, 1H), 7.89 (s,1H), 7.55-7.48 (m, 2H), 7.40 (s, 1H), 6.86 (d, J=8.7 Hz, 1H), 6.83 (dd,J=7.0, 1.6 Hz, 1H), 6.61 (dd, J=6.9, 5.1 Hz, 1H), 4.48 (d, J=5.9 Hz,2H), 4.40-4.32 (m, 2H), 3.03-2.92 (m, 2H), 2.14-2.05 (m, 2H), 1.68 (qd,J=12.5, 3.9 Hz, 2H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 7392-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}acetamide

The title compound was prepared as described in Example 1A, substitutingN-(4-aminophenyl)-2-cyclopentylacetamide for 3-methylbutan-1-amine and2-(imidazo[1,2-a]pyridin-7-yl)acetic acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, methanol-d₄) δ ppm 8.75 (dd, J=6.9, 1.0 Hz, 1H), 8.21-8.16(m, 1H), 8.01 (d, J=2.1 Hz, 1H), 7.89 (s, 1H), 7.55-7.45 (m, 5H), 3.99(s, 2H), 2.39-2.24 (m, 3H), 1.91-1.76 (m, 2H), 1.78-1.46 (m, 4H),1.39-1.15 (m, 2H); MS (ESI(+)) m/e 377 (M+H)⁺.

Example 740N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.88 (t, J=6.1 Hz, 1H),8.49 (dd, J=7.0, 0.9 Hz, 1H), 8.15 (s, 1H), 7.90-7.86 (m, 2H), 7.52 (d,J=1.2 Hz, 1H), 7.40 (s, 1H), 7.17 (d, J=3.5 Hz, 1H), 6.85 (dd, J=7.0,1.7 Hz, 1H), 6.65 (d, J=3.5 Hz, 1H), 4.49 (d, J=6.1 Hz, 2H), 3.95 (d,J=7.2 Hz, 2H), 2.21-2.05 (m, 1H), 0.85 (d, J=6.7 Hz, 6H); MS (ESI(+))m/e 364 (M+H)⁺.

Example 7415-(1-benzyl-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-benzyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.92 (t, J=6.1 Hz, 1H),8.49 (dd, J=6.9, 0.9 Hz, 1H), 8.27 (d, J=0.7 Hz, 1H), 7.93 (d, J=0.7 Hz,1H), 7.89 (t, J=0.9 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.41-7.23 (m, 6H),7.17 (d, J=3.5 Hz, 1H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 6.68 (d, J=3.5 Hz,1H), 5.39 (s, 2H), 4.49 (d, J=6.1 Hz, 2H); MS (ESI(+)) m/e 398 (M+H)⁺.

Example 742N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting(S)-1-((tetrahydrofuran-2-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.94 (t, J=6.1 Hz, 1H),8.49 (dd, J=6.9, 0.9 Hz, 1H), 8.15 (s, 1H), 7.89 (s, 2H), 7.52 (d, J=1.2Hz, 1H), 7.40 (s, 1H), 7.17 (d, J=3.5 Hz, 1H), 6.86 (dd, J=7.0, 1.7 Hz,1H), 6.68 (d, J=3.5 Hz, 1H), 4.49 (d, J=6.1 Hz, 2H), 4.28-4.09 (m, 3H),3.78-3.69 (m, 1H), 3.68-3.55 (m, 1H), 2.01-1.88 (m, 1H), 1.85-1.66 (m,2H), 1.66-1.54 (m, 1H); MS (ESI(+)) m/e 392 (M+H)⁺.

Example 743N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2R)-tetrahydrofuran-2-ylmethyl]-1H-pyrazol-4-yl}furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting(R)-1-((tetrahydrofuran-2-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.94 (t, J=6.1 Hz, 1H),8.49 (dd, J=6.9, 0.9 Hz, 1H), 8.15 (s, 1H), 7.89 (s, 2H), 7.52 (d, J=1.2Hz, 1H), 7.40 (s, 1H), 7.17 (d, J=3.5 Hz, 1H), 6.86 (dd, J=7.0, 1.7 Hz,1H), 6.68 (d, J=3.5 Hz, 1H), 4.49 (d, J=6.1 Hz, 2H), 4.28-4.07 (m, 3H),3.78-3.69 (m, 1H), 3.68-3.59 (m, 1H), 2.01-1.88 (m, 1H), 1.85-1.66 (m,2H), 1.66-1.54 (m, 1H); MS (ESI(+)) m/e 392 (M+H)⁺.

Example 744N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamideExample 744A tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)furan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline.

Example 744BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)furan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 744CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00 (t, J=5.3 Hz, 1H), 8.49 (dd, J=7.0,0.7 Hz, 1H), 7.89 (s, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.39 (s, 1H), 7.13(d, J=3.5 Hz, 1H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 6.58 (d, J=3.0 Hz, 1H),6.53 (s, 1H), 4.47 (d, J=6.1 Hz, 2H), 4.25 (s, 1H), 4.13 (s, 1H), 3.66(dd, J=12.2, 6.1 Hz, 2H), 3.01-2.82 (m, 1H), 2.47 (bs, 1H), 2.36 (bs,1H), 1.09-0.86 (m, 6H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 745N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00 (dd, J=8.8, 5.7 Hz, 1H), 8.49(dd, J=7.0, 0.5 Hz, 1H), 7.89 (s, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.39 (s,1H), 7.13 (dd, J=3.4, 2.1 Hz, 1H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 6.58(dd, J=6.2, 3.5 Hz, 1H), 6.52 (d, J=15.2 Hz, 1H), 4.47 (d, J=6.1 Hz,2H), 4.17 (dd, J=21.3, 2.5 Hz, 2H), 3.74-3.53 (m, 2H), 2.45 (bs, 1H),2.37 (bs, 1H), 2.27 (d, J=7.0 Hz, 1H), 2.22 (d, J=6.9 Hz, 1H), 2.06-1.94(m, 1H), 0.91 (dd, J=6.5, 5.3 Hz, 6H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 7465-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 8.62 (t, J=5.4 Hz, 1H), 8.44-8.39 (m, 1H),7.81 (s, 1H), 7.51-7.35 (m, 7H), 7.08 (d, J=3.5 Hz, 1H), 6.82 (dd,J=7.0, 1.6 Hz, 1H), 6.53 (d, J=3.5 Hz, 1H), 6.50-6.43 (m, 1H), 4.47 (d,J=6.1 Hz, 2H), 4.20 (d, J=2.1 Hz, 2H), 3.64 (t, J=5.3 Hz, 2H), 2.52-2.46(m, 2H); MS (ESI(+)) m/e 427 (M+H)⁺.

Example 747N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[4-(2-methylpropyl)phenyl]furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting 4-isobutylphenylboronic acid for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.08 (t, J=6.1 Hz, 1H),8.49 (dd, J=6.9, 0.8 Hz, 1H), 7.92-7.87 (m, 1H), 7.87-7.79 (m, 2H), 7.52(d, J=1.2 Hz, 1H), 7.45-7.38 (m, 1H), 7.25 (d, J=8.3 Hz, 2H), 7.21 (d,J=3.6 Hz, 1H), 7.04 (d, J=3.6 Hz, 1H), 6.87 (dd, J=7.0, 1.7 Hz, 1H),4.51 (d, J=6.0 Hz, 2H), 2.49-2.46 (m, 2H), 1.86 (dp, J=13.4, 6.8 Hz,1H), 0.87 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 374 (M+H)⁺.

Example 748N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2S)-2-methylbutanoyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and (2S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00 (t, J=5.0 Hz,1H), 8.49 (dd, J=7.0, 0.6 Hz, 1H), 7.89 (s, 1H), 7.52 (d, J=1.1 Hz, 1H),7.39 (s, 1H), 7.13 (d, J=3.5 Hz, 1H), 6.84 (dd, J=7.0, 1.6 Hz, 1H),6.61-6.56 (m, 1H), 6.53 (d, J=9.8 Hz, 1H), 4.47 (d, J=6.1 Hz, 2H),4.35-4.07 (m, 2H), 3.75-3.58 (m, 2H), 2.90-2.62 (m, 1H), 2.48-2.30 (m,2H), 1.57 (dt, J=24.3, 8.8 Hz, 1H), 1.32 (dt, J=13.1, 6.8 Hz, 1H), 0.99(dd, J=9.6, 6.8 Hz, 3H), 0.81 (q, J=7.1 Hz, 3H); MS (ESI(+)) m/e 407(M+H)⁺.

Example 7495-[1-(3,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and 3,3-dimethylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.00 (t, J=6.1 Hz,1H), 8.49 (dd, J=7.0, 0.7 Hz, 1H), 7.89 (s, 1H), 7.52 (d, J=1.2 Hz, 1H),7.39 (s, 1H), 7.13 (t, J=3.4 Hz, 1H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 6.57(dd, J=6.1, 3.6 Hz, 1H), 6.51 (d, J=23.1 Hz, 1H), 4.47 (d, J=6.0 Hz,2H), 4.19 (dd, J=31.4, 2.4 Hz, 2H), 3.73-3.62 (m, 2H), 2.41 (d, J=31.8Hz, 2H), 2.28 (d, J=17.4 Hz, 2H), 0.99 (d, J=7.2 Hz, 9H); MS (ESI(+))m/e 421 (M+H)⁺.

Example 7505-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and cyclopropylacetic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.05-8.93 (m, 1H), 8.49 (dd,J=7.0, 0.8 Hz, 1H), 7.90-7.87 (m, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.39 (bs,1H), 7.13 (d, J=3.5 Hz, 1H), 6.84 (dd, J=7.0, 1.6 Hz, 1H), 6.58 (dd,J=6.9, 3.5 Hz, 1H), 6.55-6.48 (m, 1H), 4.47 (d, J=6.1 Hz, 2H), 4.15 (d,J=8.4 Hz, 2H), 3.63 (dt, J=18.3, 5.7 Hz, 2H), 2.48-2.35 (m, 2H),2.35-2.27 (m, 2H), 1.03-0.91 (m, 1H), 0.49-0.41 (m, 2H), 0.12 (dq,J=10.2, 5.0 Hz, 2H); MS (ESI(+)) m/e 405 (M+H)⁺.

Example 751N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{1-[(2-methylpropyl)sulfonyl]pyrrolidin-3-yl}-1,3-thiazole-5-carboxamideExample 751A tert-butyl3-(5-formylthiazol-2-yl)pyrrolidine-1-carboxylate

tert-Butyl 3-carbamothioylpyrrolidine-1-carboxylate (5 g, 21.71 mmol),2-chloromalonaldehyde (3.70 g, 34.7 mmol) and magnesium carbonate (1.830g, 21.71 mmol) were combined in dioxane (100 ml). The mixture was heatedto 60° C. for 3 hours, stirred overnight at room temperature and thenfiltered through a pad of diatomaceous earth, rinsing withdichloromethane. The filtrate was concentrated in vacuo and thenpurified by normal phase chromatography to provide the title compound.

Example 751B2-(1-(tert-butoxycarbonyl)pyrrolidin-3-yl)thiazole-5-carboxylic acid

tert-Butyl 3-(5-formylthiazol-2-yl)pyrrolidine-1-carboxylate (3.65 g,12.93 mmol) was suspended in water (35 ml) and t-butanol (60 ml). Sodiumdihydrogenphosphate (2.094 g, 17.45 mmol) was added, followed by2-methylbut-2-ene (5.34 ml, 50.4 mmol). After 5 minutes, sodium chlorite(2.92 g, 32.3 mmol) was added in portions over about 5 minutes (mildlyexothermic). The reaction was stirred for 1 hour at room temperature,then additional 2-methyl-2-butene (2 mL) was added. After stirring for 2hours at room temperature, the reaction was concentrated and water (100mL) was added. The mixture was adjusted to pH 2 by addition of 1Nhydrochloric acid, then extracted dichloromethane. The organic extractswere dried over sodium sulfate, filtered and concentrated to provide thetitle compound.

Example 751C tert-butyl3-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiazol-2-yl)pyrrolidine-1-carboxylate

The title compound was prepared as described in Example 688D,substituting2-(1-(tert-butoxycarbonyl)pyrrolidin-3-yl)thiazole-5-carboxylic acid forlithium 2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate.

Example 751DN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl3-(5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiazol-2-yl)pyrrolidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 751EN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-{1-[(2-methylpropyl)sulfonyl]pyrrolidin-3-yl}-1,3-thiazole-5-carboxamide

N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamide,2.7-trifluoroacetic acid (150 mg, 0.236 mmol) was dissolved inN,N-dimethylformamide (0.7 mL). Triethylamine (0.3 mL, 2.152 mmol) wasadded, followed by 2-methylpropane-1-sulfonyl chloride (74.0 mg, 0.472mmol) and the reaction was stirred overnight at room temperature. Thereaction mixture was diluted with water and extracted with ethylacetate. The organic extracts were dried with sodium sulfate, filtered,and concentrated and purified by normal phase chromatography to give thetitle compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.24 (t, J=5.9 Hz, 1H),8.49 (d, J=7.0 Hz, 1H), 8.35 (s, 1H), 7.89 (s, 1H), 7.52 (d, J=1.2 Hz,1H), 7.41 (s, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 4.48 (d, J=5.9 Hz, 2H),3.91 (p, J=7.2 Hz, 1H), 3.74 (dd, J=9.8, 7.3 Hz, 1H), 3.51-3.35 (m, 3H),2.99 (d, J=6.6 Hz, 2H), 2.46-2.33 (m, 1H), 2.24-2.03 (m, 2H), 1.03 (d,J=6.7 Hz, 6H); MS (ESI(+)) m/e 448 (M+H)⁺.

Example 752N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(phenylsulfonyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 682,substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamidefor N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.20 (t, J=5.9 Hz, 1H), 8.50 (dd, J=7.0,0.9 Hz, 1H), 8.21 (s, 1H), 7.89 (t, J=0.9 Hz, 1H), 7.84-7.77 (m, 2H),7.74-7.65 (m, 1H), 7.65-7.57 (m, 2H), 7.52 (d, J=1.2 Hz, 1H), 7.40 (bs,1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 4.47 (d, J=5.9 Hz, 2H), 3.80-3.59 (m,2H), 3.44-3.31 (m, 3H), 2.32-2.17 (m, 1H), 2.06-1.93 (m, 1H); MS(ESI(+)) m/e 468 (M+H)⁺.

Example 753N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(2-methylpropyl)sulfonyl]-1,2,3,6-tetrahydropyridin-4-yl}furan-2-carboxamide

The title compound was prepared as described in Example 682,substituting 2-methylpropane sulfonyl chloride for benzenesulfonylchloride andN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 9.04-8.96 (m, 1H), 8.48 (dd, J=6.9, 0.9 Hz,1H), 7.89-7.87 (m, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.39 (s, 1H), 7.13 (d,J=3.5 Hz, 1H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 6.62-6.57 (m, 1H),6.56-6.51 (m, 1H), 4.47 (d, J=6.1 Hz, 2H), 3.97-3.91 (m, 2H), 3.40 (t,J=5.7 Hz, 2H), 2.97 (d, J=6.5 Hz, 2H), 2.54-2.48 (m, 2H), 2.19-2.05 (m,1H), 1.07-1.01 (m, 6H); MS (ESI(+)) m/e 443 (M+H)⁺.

Example 754N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and5-(1-isobutyl-1H-pyrazol-4-yl)thiophene-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.10-9.01 (m, 2H),8.53 (d, J=1.3 Hz, 1H), 8.18-8.16 (m, 1H), 8.14 (d, J=0.5 Hz, 1H),7.83-7.79 (m, 2H), 7.76 (d, J=3.9 Hz, 1H), 7.22 (d, J=3.9 Hz, 1H), 4.54(d, J=5.7 Hz, 2H), 3.92 (d, J=7.2 Hz, 2H), 2.13 (dp, J=13.6, 6.7 Hz,1H), 0.85 (d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 381 (M+H)⁺.

Example 755 tert-butyl4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidine-1-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-methyl-4-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)methyl)piperidine-1-carboxylatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.02 (t, J=6.0 Hz,1H), 8.49 (dd, J=7.0, 0.8 Hz, 1H), 8.13 (s, 1H), 7.91-7.86 (m, 1H), 7.81(d, J=0.4 Hz, 1H), 7.74 (d, J=3.9 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.40(s, 1H), 7.23 (d, J=3.8 Hz, 1H), 6.84 (dd, J=7.0, 1.7 Hz, 1H), 4.48 (d,J=5.8 Hz, 2H), 4.02 (s, 2H), 3.65-3.50 (m, 2H), 3.19-3.02 (m, 2H),1.47-1.34 (m, 11H), 1.30-1.15 (m, 2H), 0.93 (s, 3H); MS (ESI(+)) m/e 535(M+H)⁺.

Example 789N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.¹H NMR (500 MHz, DMSO-d₆) δ ppm 14.80 (s, 1H), 9.65 (t, J=6.0 Hz, 1H),9.20 (s, 1H), 8.99 (s, 1H), 8.91 (d, J=7.0 Hz, 1H), 8.36 (d, J=2.0 Hz,1H), 8.21 (s, 1H), 8.17 (d, J=2.1 Hz, 1H), 7.96 (d, J=3.9 Hz, 1H), 7.86(s, 1H), 7.84 (s, 1H), 7.51 (dd, J=7.0, 1.4 Hz, 1H), 7.28 (d, J=3.8 Hz,1H), 4.64 (d, J=5.8 Hz, 2H), 4.10 (s, 2H), 3.19-3.12 (m, 2H), 3.04-2.96(m, 2H), 1.74-1.59 (m, 2H), 1.57-1.46 (m, 2H), 0.96 (s, 3H); MS (ESI(+))m/e 435 (M+H)⁺.

Example 7905-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-fluorotetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.97 (t, J=6.1 Hz, 1H),8.50 (dd, J=13.4, 3.5 Hz, 1H), 8.16 (s, 1H), 7.94 (s, 1H), 7.92 (s, 1H),7.56 (d, J=1.1 Hz, 1H), 7.43 (s, 1H), 7.18 (d, J=3.5 Hz, 1H), 6.89 (dd,J=7.0, 1.5 Hz, 1H), 6.71 (d, J=6.4 Hz, 1H), 4.51 (d, J=6.1 Hz, 2H), 4.46(d, J=21.9 Hz, 2H), 3.81-3.70 (m, 2H), 3.56-3.45 (m, 2H), 1.89-1.68 (m,2H), 1.53 (t, J=11.7 Hz, 2H); MS (ESI(+)) m/e 424 (M+H)⁺.

Example 801N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(phenylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 682,substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹HNMR (300 MHz, DMSO-d₆) δ ppm 8.97 (t, J=6.1 Hz, 1H), 8.47 (d, J=6.5 Hz,1H), 7.88 (s, 1H), 7.85-7.78 (m, 2H), 7.75-7.68 (m, 1H), 7.69-7.60 (m,2H), 7.51 (d, J=1.2 Hz, 1H), 7.37 (s, 1H), 7.10 (d, J=3.5 Hz, 1H), 6.82(dd, J=7.0, 1.7 Hz, 1H), 6.54 (d, J=3.5 Hz, 1H), 6.46-6.43 (m, 1H), 4.46(d, J=6.1 Hz, 2H), 3.79-3.74 (m, 2H), 3.28-3.21 (m, 2H), 2.45 (s, 2H);MS (ESI(+)) m/e 463 (M+H)⁺.

Example 8022-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 52A,substituting 2-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(piperidin-4-yl)thiazole-5-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.23 (t,J=5.9 Hz, 1H), 8.49 (d, J=6.9 Hz, 1H), 8.34 (s, 1H), 7.89 (s, 1H),7.56-7.36 (m, 4H), 7.35-7.25 (m, 2H), 6.84 (dd, J=7.0, 1.7 Hz, 1H),4.61-4.52 (m, 1H), 4.48 (d, J=5.9 Hz, 2H), 3.51-3.39 (m, 1H), 3.42-3.34(m, 1H), 3.23 (t, J=12.1 Hz, 1H), 3.01 (td, J=12.7, 2.9 Hz, 1H),2.21-2.13 (m, 1H), 2.08-1.97 (m, 1H), 1.77-1.54 (m, 2H); MS (ESI(+)) m/e464 (M+H)⁺.

Example 8035-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)furan-2-carboxamidefor 3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.66-8.58 (m, 1H), 8.45-8.39 (m,1H), 7.81 (s, 1H), 7.54-7.44 (m, 2H), 7.43-7.36 (m, 2H), 7.31-7.21 (m,2H), 7.08 (d, J=3.5 Hz, 1H), 6.82 (dd, J=6.9, 1.7 Hz, 1H), 6.53 (d,J=3.4 Hz, 1H), 6.48 (bs, 1H), 4.47 (d, J=6.1 Hz, 2H), 4.41-3.34 (m, 4H),2.52-2.37 (m, 2H); MS (ESI(+)) m/e 445 (M+H)⁺.

Example 8042-[1-(2-fluorobenzoyl)pyrrolidin-3-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.95-8.88 (m, 1H), 8.43 (d, J=7.0Hz, 1H), 8.32-8.17 (m, 1H), 7.82 (s, 1H), 7.53-7.35 (m, 4H), 7.30-7.19(m, 2H), 6.85-6.78 (m, 1H), 4.50-4.44 (m, 2H), 4.05-3.23 (m, 5H),2.45-2.11 (m, 2H); MS (ESI(+)) m/e 450 (M+H)⁺.

Example 805N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(2-methylpropanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.28-9.19 (m, 1H), 8.49 (dd, J=6.9, 0.9Hz, 1H), 8.34 (d, J=2.4 Hz, 1H), 7.91-7.87 (m, 1H), 7.52 (d, J=1.2 Hz,1H), 7.41 (s, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 4.48 (d, J=5.9 Hz, 2H),4.11-3.33 (m, 5H), 3.17 (d, J=5.2 Hz, 1H), 2.74-2.59 (m, 1H), 2.46-2.00(m, 6H), 1.03-0.97 (m, 1H); MS (ESI(+)) m/e 398 (M+H)⁺.

Example 806N-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-[1-(3-methylbutanoyl)pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.28-9.19 (m, 1H), 8.49 (d, J=7.0Hz, 1H), 8.34 (d, J=2.4 Hz, 1H), 7.91-7.87 (m, 1H), 7.52 (d, J=1.2 Hz,1H), 7.43-7.38 (m, 1H), 6.83 (dd, J=7.0, 1.7 Hz, 1H), 4.48 (d, J=5.9 Hz,2H), 3.97-3.72 (m, 2H), 3.70-3.46 (m, 2H), 3.17 (d, J=5.1 Hz, 1H),2.45-1.91 (m, 5H), 0.94-0.86 (m, 6H); MS (ESI(+)) m/e 412 (M+H)⁺.

Example 8072-(1-benzoylpyrrolidin-3-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyridin-7-ylmethyl)-2-(pyrrolidin-3-yl)thiazole-5-carboxamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 8.94-8.87 (m, 1H), 8.43 (d, J=6.9 Hz, 1H),8.27 (s, 1H), 8.23-8.16 (m, 1H), 7.82 (s, 1H), 7.52-7.38 (m, 6H), 6.81(dd, J=6.9, 1.7 Hz, 1H), 4.47 (d, J=5.8 Hz, 2H), 3.94-3.84 (m, 2H),3.76-3.53 (m, 3H), 2.44-2.34 (m, 1H), 2.24-2.14 (m, 1H); MS (ESI(+)) m/e432 (M+H)⁺.

Example 808 tert-butyl4-[2-(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)ethyl]piperazine-1-carboxylateExample 808A tert-butyl4-(2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylate

4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (0.500 g,2.58 mmol), tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate (0.593g, 2.58 mmol) and 2-(tributylphosphoranylidene)acetonitrile (0.746 g,3.09 mmol) were stirred together in toluene (10 ml) at 85° C. overnight.The reaction was concentrated and purified by normal phasechromatography to give the title compound.

Example 808B tert-butyl4-[2-(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)ethyl]piperazine-1-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.02 (t, J=6.0 Hz,1H), 8.53-8.45 (m, 1H), 8.16 (s, 1H), 7.89 (d, J=0.7 Hz, 1H), 7.79 (d,J=0.5 Hz, 1H), 7.74 (d, J=3.8 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.39 (s,1H), 7.22 (d, J=3.9 Hz, 1H), 6.84 (dd, J=7.0, 1.6 Hz, 1H), 4.48 (d,J=5.9 Hz, 2H), 4.23 (t, J=6.5 Hz, 2H), 3.29-3.25 (m, 2H), 2.74 (t, J=6.6Hz, 2H), 2.42-2.33 (m, 4H), 1.38 (s, 9H); MS (ESI(+)) m/e 536 (M+H)⁺.

Example 809N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-[2-(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)ethyl]piperazine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.34 (t, J=5.9 Hz, 1H), 8.94 (s, 2H),8.87 (d, J=7.0 Hz, 1H), 8.33 (dd, J=2.1, 0.7 Hz, 1H), 8.22 (d, J=0.8 Hz,1H), 8.15 (d, J=2.1 Hz, 1H), 7.87 (d, J=0.8 Hz, 1H), 7.82 (d, J=3.9 Hz,1H), 7.79 (s, 1H), 7.47 (dd, J=7.0, 1.5 Hz, 1H), 7.27 (d, J=3.8 Hz, 1H),4.65 (d, J=5.9 Hz, 2H), 4.43-4.34 (m, 2H), 3.22-3.16 (m, 6H), 2.98-2.89(m, 4H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 8105-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamideExample 810AN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromofuran-2-carboxamide

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amineand 5-bromofuran-2-carboxylic acid for 4-nitrobenzoic acid.

Example 810B5-{1-[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-fluorotetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromofuran-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.93 (t, J=6.0 Hz,1H), 8.90-8.85 (m, 1H), 8.48 (s, 1H), 8.13 (s, 1H), 7.92 (d, J=0.5 Hz,1H), 7.84 (dd, J=9.2, 0.7 Hz, 1H), 7.66 (dd, J=9.2, 1.7 Hz, 1H), 7.16(d, J=3.6 Hz, 1H), 6.70 (d, J=3.5 Hz, 1H), 4.56 (d, J=6.0 Hz, 2H), 4.45(d, J=21.8 Hz, 2H), 3.82-3.66 (m, 2H), 3.51 (td, J=11.2, 2.0 Hz, 2H),1.92-1.63 (m, 2H), 1.60-1.42 (m, 2H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 811N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamideExample 811AN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-{4-[(imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 811BN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (500 MHz, methanol-d₄) δ ppm 9.24 (s, 1H), 8.72-8.68 (m, 1H),8.27-8.23 (m, 1H), 8.11-8.07 (m, 1H), 7.88-7.82 (m, 2H), 7.41-7.35 (m,2H), 4.76 (s, 2H), 4.75-4.66 (m, 1H), 4.24-4.15 (m, 1H), 3.29-3.18 (m,1H), 3.06-2.85 (m, 2H), 2.78-2.64 (m, 1H), 2.02-1.84 (m, 2H), 1.74-1.52(m, 2H), 1.17-1.07 (m, 6H); MS (ESI(+)) m/e 406 (M+H)⁺.

Example 8124-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 4-fluorobenzoic acid for 4-nitrobenzoic acid.¹H NMR (500 MHz, methanol-d₄) δ ppm 9.29-9.25 (m, 1H), 8.72 (d, J=1.4Hz, 1H), 8.27 (d, J=1.7 Hz, 1H), 8.12 (d, J=1.7 Hz, 1H), 7.89-7.83 (m,2H), 7.55-7.45 (m, 2H), 7.44-7.38 (m, 2H), 7.25-7.16 (m, 2H), 4.87-4.84(m, 1H), 4.77 (s, 2H), 3.90-3.79 (m, 1H), 3.33-3.19 (m, 1H), 3.03-2.89(m, 2H), 2.07-1.61 (m, 4H); MS (ESI(+)) m/e 458 (M+H)⁺.

Example 8134-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 2,5-difluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (500 MHz, methanol-d₄) δ ppm 9.23 (s, 1H), 8.69 (s, 1H),8.24 (d, J=1.6 Hz, 1H), 8.07 (d, J=1.6 Hz, 1H), 7.89-7.83 (m, 2H),7.43-7.36 (m, 2H), 7.31-7.15 (m, 3H), 4.84-4.73 (m, 3H), 3.71-3.62 (m,1H), 3.36-3.24 (m, 1H), 3.04-2.90 (m, 2H), 2.04-1.95 (m, 1H), 1.92-1.61(m, 3H); MS (ESI(+)) m/e 476 (M+H)⁺.

Example 814N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 1-methylcyclopropanecarboxylic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, methanol-d₄) δ ppm 9.28 (s, 1H),8.73 (s, 1H), 8.28 (d, J=1.7 Hz, 1H), 8.13 (d, J=1.7 Hz, 1H), 7.89-7.83(m, 2H), 7.42-7.36 (m, 2H), 4.78 (s, 2H), 4.62-4.53 (m, 2H), 3.20-2.70(m, 3H), 1.97-1.89 (m, 2H), 1.72-1.57 (m, 2H), 1.33 (s, 3H), 0.96-0.89(m, 2H), 0.71-0.58 (m, 2H); MS (ESI(+)) m/e 418 (M+H)⁺.

Example 815N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 3,3,3-trifluoropropanoic acid for4-nitrobenzoic acid. ¹H NMR (500 MHz, methanol-d₄) δ ppm 9.22 (d, J=1.4Hz, 1H), 8.68 (d, J=1.4 Hz, 1H), 8.23 (d, J=1.9 Hz, 1H), 8.06 (d, J=1.6Hz, 1H), 7.89-7.82 (m, 2H), 7.42-7.34 (m, 2H), 4.81-4.65 (m, 3H),4.11-3.99 (m, 1H), 3.62-3.44 (m, 2H), 3.37-3.21 (m, 1H), 3.01-2.86 (m,1H), 2.85-2.71 (m, 1H), 1.99-1.85 (m, 2H), 1.85-1.54 (m, 2H); MS(ESI(+)) m/e 446 (M+H)⁺.

Example 816N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3-methylbutanoyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoic acid.¹H NMR (500 MHz, methanol-d₄) δ ppm 99.24 (d, J=1.4 Hz, 1H), 8.70 (d,J=1.4 Hz, 1H), 8.25 (d, J=1.7 Hz, 1H), 8.09 (d, J=1.7 Hz, 1H), 7.89-7.82(m, 2H), 7.41-7.34 (m, 2H), 4.79-4.66 (m, 3H), 4.19-4.07 (m, 1H),3.30-3.16 (m, 1H), 3.00-2.85 (m, 1H), 2.80-2.63 (m, 1H), 2.36-2.29 (m,2H), 2.17-2.00 (m, 1H), 2.01-1.84 (m, 2H), 1.75-1.50 (m, 2H), 0.99 (d,J=6.6 Hz, 6H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 817N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(propan-2-ylsulfonyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 682,substituting propane-2-sulfonyl chloride for benzenesulfonyl chlorideand N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide forN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹H NMR(500 MHz, methanol-d₄) δ ppm 9.21 (d, J=1.4 Hz, 1H), 8.67 (d, J=1.4 Hz,1H), 8.22 (d, J=1.6 Hz, 1H), 8.05 (d, J=1.6 Hz, 1H), 7.89-7.82 (m, 2H),7.40-7.35 (m, 2H), 4.85-4.79 (m, 1H), 4.75 (s, 2H), 3.96-3.85 (m, 2H),3.12-3.00 (m, 2H), 2.88-2.74 (m, 1H), 1.95-1.85 (m, 2H), 1.84-1.65 (m,2H), 1.33 (d, J=6.8 Hz, 6H); MS (ESI(+)) m/e 442 (M+H)⁺.

Example 818N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-isobutyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=6.1 Hz, 1H),8.49 (dd, J=7.0, 0.7 Hz, 1H), 7.89 (s, 1H), 7.54-7.51 (m, 2H), 7.41 (s,1H), 7.30 (d, J=3.6 Hz, 1H), 6.96 (d, J=3.6 Hz, 1H), 6.85 (dd, J=7.0,1.6 Hz, 1H), 6.76 (d, J=1.9 Hz, 1H), 4.50 (d, J=6.0 Hz, 2H), 4.22 (d,J=7.3 Hz, 2H), 2.04 (dp, J=13.8, 6.8 Hz, 1H), 0.81 (d, J=6.7 Hz, 6H); MS(ESI(+)) m/e 364 (M+H)⁺.

Example 819N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamideExample 819A 5-(1-isobutyl-1H-pyrazol-4-yl)furan-2-carboxylic acid

The title compound was prepared as described in Example 51A,substituting 5-bromofuran-2-carboxylic acid for 4-bromoaniline.

Example 819BN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]furan-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and5-(1-isobutyl-1H-pyrazol-4-yl)furan-2-carboxylic acid for 4-nitrobenzoicacid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.05-9.02 (m, 1H), 8.90 (t, J=6.0Hz, 1H), 8.52 (d, J=1.4 Hz, 1H), 8.19-8.14 (m, 2H), 7.90-7.88 (m, 1H),7.80 (d, J=1.0 Hz, 1H), 7.17 (d, J=3.5 Hz, 1H), 6.65 (d, J=3.5 Hz, 1H),4.56 (d, J=5.9 Hz, 2H), 3.96 (d, J=7.1 Hz, 2H), 2.20-2.07 (m, 1H), 0.85(d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 365 (M+H)⁺.

Example 8205-[1-(2-methylpropyl)-1H-pyrazol-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amineand 5-(1-isobutyl-1H-pyrazol-4-yl)furan-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.94-8.85 (m, 2H),8.48 (s, 1H), 8.14 (s, 1H), 7.87 (s, 1H), 7.84 (d, J=9.1 Hz, 1H), 7.66(dd, J=9.1, 1.7 Hz, 1H), 7.16 (d, J=3.5 Hz, 1H), 6.64 (d, J=3.5 Hz, 1H),4.56 (d, J=6.0 Hz, 2H), 3.95 (d, J=7.1 Hz, 2H), 2.21-1.97 (m, 1H),0.90-0.76 (m, 6H); MS (ESI(+)) m/e 365 (M+H)⁺.

Example 821N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(3-methylbutyl)-1H-pyrazol-5-yl]furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting 1-isopentyl-1H-pyrazol-5-ylboronic acid for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.03 (t, J=6.1 Hz, 1H),8.49 (dd, J=7.0, 0.8 Hz, 1H), 7.89 (s, 1H), 7.58-7.43 (m, 2H), 7.43-7.37(m, 1H), 7.30 (d, J=3.5 Hz, 1H), 6.95 (d, J=3.6 Hz, 1H), 6.85 (dd,J=7.0, 1.7 Hz, 1H), 6.73 (d, J=1.9 Hz, 1H), 4.50 (d, J=6.0 Hz, 2H),4.44-4.36 (m, 2H), 1.68-1.38 (m, 3H), 0.84 (d, J=6.4 Hz, 6H); MS(ESI(+)) m/e 378 (M+H)⁺.

Example 8225-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-methyltetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-bromofuran-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.95-8.83 (m, 2H),8.48 (s, 1H), 8.15-8.09 (m, 1H), 7.88 (d, J=0.4 Hz, 1H), 7.83 (dd,J=9.2, 0.7 Hz, 1H), 7.66 (dd, J=9.2, 1.7 Hz, 1H), 7.16 (d, J=3.5 Hz,1H), 6.66 (d, J=3.5 Hz, 1H), 4.56 (d, J=6.0 Hz, 2H), 4.06 (s, 2H), 3.68(dt, J=11.4, 4.5 Hz, 2H), 3.51 (ddd, J=11.9, 9.3, 2.9 Hz, 2H), 1.50(ddd, J=13.4, 9.2, 4.2 Hz, 2H), 1.31-1.17 (m, 2H), 0.96 (s, 3H); MS(ESI(+)) m/e 421 (M+H)⁺.

Example 823N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamideExample 823A Methyl5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophene-2-carboxylate

The title compound was prepared as described in Example 688D,substituting 5-(methoxycarbonyl)thiophene-2-carboxylic acid for lithium2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate.

Example 823B Lithium5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophene-2-carboxylate

The title compound was prepared as described in Example 688C,substituting methyl5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophene-2-carboxylate forethyl 2-(1-phenylpiperidin-4-yl)thiazole-5-carboxylate.

Example 823CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A,substituting), (R)-2-(methoxymethyl)pyrrolidine for3-methylbutan-1-amine and lithium5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophene-2-carboxylate for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.23 (t, J=6.0 Hz,1H), 8.49 (dd, J=6.9, 0.9 Hz, 1H), 7.90-7.88 (m, 1H), 7.79 (d, J=4.0 Hz,1H), 7.60 (d, J=4.0 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.42-7.39 (m, 1H),6.85 (dd, J=7.0, 1.7 Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.35-4.23 (m, 1H),3.78-3.65 (m, 2H), 3.26 (s, 3H), 2.02-1.81 (m, 4H); MS (ESI(+)) m/e 399(M+H)⁺.

Example 824N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A,substituting), 2-isobutylpyrrolidine for 3-methylbutan-1-amine andlithium5-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)thiophene-2-carboxylate for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.23 (t, J=6.0 Hz,1H), 8.49 (dd, J=6.9, 0.9 Hz, 1H), 7.90-7.88 (m, 1H), 7.79 (d, J=4.0 Hz,1H), 7.60 (d, J=4.0 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.42-7.39 (m, 1H),6.85 (dd, J=7.0, 1.7 Hz, 1H), 4.49 (d, J=5.9 Hz, 2H), 4.35-4.23 (m, 1H),3.78-3.65 (m, 2H), 3.26 (s, 3H), 2.02-1.81 (m, 4H); MS (ESI(+)) m/e 411(M+H)⁺.

Example 8255-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-neopentyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.89 (t, J=6.1 Hz, 1H),8.49 (dd, J=7.0, 0.9 Hz, 1H), 8.11 (d, J=0.5 Hz, 1H), 7.95-7.83 (m, 2H),7.52 (d, J=1.2 Hz, 1H), 7.46-7.34 (m, 1H), 7.17 (d, J=3.4 Hz, 1H), 6.85(dd, J=7.0, 1.7 Hz, 1H), 6.66 (d, J=3.5 Hz, 1H), 4.49 (d, J=6.0 Hz, 2H),3.95 (s, 2H), 0.92 (s, 9H); MS (ESI(+)) m/e 378 (M+H)⁺.

Example 8264-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide for3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoic acid.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.08-9.00 (m, 2H), 8.49 (d, J=1.4 Hz,1H), 8.16-8.13 (m, 1H), 7.92-7.85 (m, 2H), 7.79 (d, J=1.0 Hz, 1H),7.57-7.23 (m, 6H), 4.74-4.61 (m, 1H), 4.57 (d, J=5.7 Hz, 2H), 3.54-3.43(m, 1H), 3.24-3.14 (m, 1H), 3.00-2.79 (m, 2H), 1.97-1.84 (m, 1H),1.82-1.47 (m, 3H); MS (ESI(+)) m/e 458 (M+H)⁺.

Example 8275-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamideExample 827A tert-butyl4-(5-(ethoxycarbonyl)thiophen-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand ethyl 5-bromothiophene-2-carboxylate for 4-bromoaniline.

Example 827B tert-butyl4-(5-(ethoxycarbonyl)thiophen-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1B, substitutingtert-butyl 4-(5-(ethoxycarbonyl)thiophen-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for N-isopentyl-4-nitrobenzamide.

Example 827C5-(1-(tert-butoxycarbonyl)piperidin-4-yl)thiophene-2-carboxylic acid

In a 250 mL round bottom flask was mixed tert-butyl4-(5-(ethoxycarbonyl)thiophen-2-yl)piperidine-1-carboxylate (5.00 g,14.73 mmol) in tetrahydrofuran (50 ml). Aqueous 4N NaOH (38.41 ml, 73.6mmol) solution was added along with some methanol (10 ml) to get asingle phase solution. The mixture was stirred overnight at roomtemperature. The solvents were removed to give a white slurry that wasdiluted with water and adjusted to pH of 5 with 1N aqueous hydrochloricacid. Filtration provided the title compound.

Example 827D tert-butyl4-(5-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)thiophen-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and5-(1-(tert-butoxycarbonyl)piperidin-4-yl)thiophene-2-carboxylic acid for4-nitrobenzoic acid.

Example 827EN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)thiophen-2-yl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 827F5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.05 (m,2H), 8.50 (d, J=1.5 Hz, 1H), 8.16 (s, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69(d, J=3.7 Hz, 1H), 7.50 (m, 1H), 7.43 (m, 1H), 7.31 (m, 2H), 6.98 (d,J=3.8 Hz, 1H), 4.60 (m, 1H), 4.52 (d, J=5.8 Hz, 2H), 3.45 (m, 1H), 3.18(m, 2H), 2.93 (m, 1H), 2.12-1.85 (m, 2H), 1.52 (m, 2H); MS (ESI(+)) m/e464 (M+H)⁺.

Example 8285-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 4-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.05 (m,2H), 8.51 (d, J=1.4 Hz, 1H), 8.16 (t, J=0.8 Hz, 1H), 7.80 (d, J=1.0 Hz,1H), 7.70 (d, J=3.8 Hz, 1H), 7.49 (m, 2H), 7.28 (m, 2H), 6.99 (dd,J=3.7, 0.8 Hz, 1H), 4.54 (m, 1H), 4.52 (d, J=5.8 Hz, 2H), 3.65 (m, 1H),3.15 (m, 2H), 2.93 (m, 1H), 1.97 (m, 2H), 1.59 (m, 2H); MS (ESI(+)) m/e464 (M+H)⁺.

Example 8295-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2,4-difluorobenzoyl chloride for 2-cyclopentylacetylchloride andN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.05 (m,2H), 8.50 (d, J=1.4 Hz, 1H), 8.16 (s, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69(d, J=3.8 Hz, 1H), 7.52 (m, 1H), 7.37 (td, J=9.7, 2.4 Hz, 1H), 7.19 (td,J=8.5, 2.5 Hz, 1H), 6.98 (d, J=3.8 Hz, 1H), 4.58 (m, 1H), 4.52 (d, J=5.8Hz, 2H), 3.43 (m, 1H), 3.17 (m, 2H), 2.92 (m, 1H), 2.00 (m, 2H), 1.52(m, 2H); MS (ESI(+)) m/e 482 (M+H)⁺.

Example 8305-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2,5-difluorobenzoyl chloride for 2-cyclopentylacetylchloride andN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.04 (m,2H), 8.51 (d, J=1.5 Hz, 1H), 8.16 (s, 1H), 7.80 (d, J=1.1 Hz, 1H), 7.70(d, J=3.8 Hz, 1H), 7.56 (m, 1H), 7.36 (m, 2H), 6.98 (d, J=3.8 Hz, 1H),4.57 (m, 1H), 4.52 (d, J=5.8 Hz, 2H), 3.46 (m, 1H), 3.17 (m, 2H), 2.93(m, 1H), 2.02 (m, 2H), 1.55 (m, 2H); MS (ESI(+)) m/e 482 (M+H)⁺.

Example 8315-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamideExample 831A tert-butyl4-(5-(([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)carbamoyl)thiophen-2-yl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amineand 5-(1-(tert-butoxycarbonyl)piperidin-4-yl)thiophene-2-carboxylic acidfor 4-nitrobenzoic acid.

Example 831BN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(5-(([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)carbamoyl)thiophen-2-yl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 831C5-[1-(2-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (t,J=5.9 Hz, 1H), 8.86 (d, J=1.5 Hz, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1,0.9 Hz, 1H), 7.64 (m, 2H), 7.50 (m, 1H), 7.42 (m, 1H), 7.31 (m, 2H),6.97 (dd, J=3.7, 0.8 Hz, 1H), 4.60 (m, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.45(m, 1H), 3.17 (m, 2H), 2.93 (m, 1H), 2.07 (m, 1H), 1.93 (m, 1H), 1.54(m, 2H); MS (ESI(+)) m/e 464 (M+H)⁺.

Example 8325-[1-(3-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 3-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t,J=5.9 Hz, 1H), 8.86 (d, J=1.5 Hz, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1,0.9 Hz, 1H), 7.66 (m, 2H), 7.50 (m, 1H), 7.34-7.22 (m, 3H), 6.98 (d,J=3.8 Hz, 1H), 4.55 (m, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.56 (m, 1H), 3.13(m, 2H), 2.91 (m, 1H), 1.97 (m, 2H), 1.60 (m, 2H); MS (ESI(+)) m/e 464(M+H)⁺.

Example 8335-[1-(4-fluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 4-fluorobenzoyl chloride for 2-cyclopentylacetyl chlorideandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t,J=5.9 Hz, 1H), 8.86 (d, J=1.5 Hz, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1,0.9 Hz, 1H), 7.64 (m, 2H), 7.47 (m, 2H), 7.27 (m, 2H), 6.98 (dd, J=3.7,0.8 Hz, 1H), 4.55 (m, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.62 (m, 1H), 3.14(m, 2H), 2.91 (m, 1H), 1.97 (m, 2H), 1.58 (m, 2H); MS (ESI(+)) m/e 464(M+H)⁺.

Example 8345-[1-(2,4-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2,4-difluorobenzoyl chloride for 2-cyclopentylacetylchloride andN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t,J=5.9 Hz, 1H), 8.86 (m, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H),7.64 (m, 2H), 7.52 (m, 1H), 7.36 (td, J=9.7, 2.4 Hz, 1H), 7.19 (m, 1H),6.97 (dd, J=3.8, 0.8 Hz, 1H), 4.57 (m, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.46(m, 1H), 3.18 (m, 2H), 2.92 (m, 1H), 2.07 (m, 1H), 1.93 (m, 1H), 1.52(m, 2H); MS (ESI(+)) m/e 482 (M+H)⁺.

Example 8355-[1-(2,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 2,5-difluorobenzoyl chloride for 2-cyclopentylacetylchloride andN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t,J=5.9 Hz, 1H), 8.86 (d, J=1.5 Hz, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1,0.9 Hz, 1H), 7.64 (m, 2H), 7.37 (m, 3H), 6.97 (dd, J=3.7, 0.8 Hz, 1H),4.57 (m, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.46 (m, 1H), 3.19 (m, 2H), 2.93(m, 1H), 2.13 (m, 1H), 1.92 (m, 1H), 1.54 (m, 2H); MS (ESI(+)) m/e 482(M+H)⁺.

Example 8365-[1-(3,5-difluorobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 52A,substituting 3,5-difluorobenzoyl chloride for 2-cyclopentylacetylchloride andN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor methyl 4-aminobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t,J=5.9 Hz, 1H), 8.86 (d, J=1.5 Hz, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1,0.9 Hz, 1H), 7.64 (m, 2H), 7.34 (tt, J=9.4, 2.4 Hz, 1H), 7.19 (m, 2H),6.98 (dd, J=3.8, 0.8 Hz, 1H), 4.55 (m, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.55(m, 1H), 3.15 (m, 2H), 2.90 (m, 1H), 2.03 (m, 1H), 1.90 (m, 1H), 1.61(m, 2H); MS (ESI(+)) m/e 482 (M+H)⁺.

Example 837N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(2-methylpropanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (m, 2H), 8.50 (d, J=1.4 Hz, 1H),8.16 (m, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69 (d, J=3.8 Hz, 1H), 6.96 (dd,J=3.7, 0.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H), 4.49 (m, 1H), 4.02 (m, 1H),3.13 (m, 2H), 2.90 (m, 1H), 2.64 (m, 1H), 1.99 (m, 2H), 1.43 (m, 2H),1.00 (m, 6H); MS (ESI(+)) m/e 412 (M+H)⁺.

Example 838N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(3-methylbutanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (m, 2H), 8.50 (d, J=1.4 Hz,1H), 8.16 (s, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69 (d, J=3.8 Hz, 1H), 6.96(dd, J=3.7, 0.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H), 4.49 (m, 1H), 3.96 (m,1H), 3.10 (m, 2H), 2.64 (m, 1H), 2.21 (d, J=7.0 Hz, 2H), 1.99 (m, 3H),1.43 (m, 2H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 426 (M+H)⁺.

Example 839N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (1-methylcyclopropyl)carboxylic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (m, 2H), 8.50(d, J=1.4 Hz, 1H), 8.16 (d, J=0.9 Hz, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69(d, J=3.8 Hz, 1H), 6.97 (dd, J=3.7, 0.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H),4.33 (m, 2H), 3.11 (m, 1H), 2.93 (m, 2H), 1.99 (m, 2H), 1.47 (m, 2H),1.23 (s, 3H), 0.80 (m, 2H), 0.54 (m, 2H); MS (ESI(+)) m/e 424 (M+H)⁺.

Example 840N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 4,4,4-trifluorobutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (m, 2H), 8.50(d, J=1.4 Hz, 1H), 8.16 (s, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69 (d, J=3.8Hz, 1H), 6.96 (dd, J=3.7, 0.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H), 4.47 (m,1H), 3.94 (m, 1H), 3.13 (m, 2H), 2.66 (m, 3H), 2.50 (m, 2H), 1.97 (m,2H), 1.57 (m, 1H), 1.41 (m, 1H); MS (ESI(+)) m/e 466 (M+H)⁺.

Example 841N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and tetrahydro-2H-pyran-4-ylcarboxylic acidfor 4-nitrobenzoic acid. 1H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (m, 2H),8.50 (d, J=1.4 Hz, 1H), 8.16 (s, 1H), 7.80 (d, J=1.0 Hz, 1H), 7.69 (d,J=3.8 Hz, 1H), 6.96 (dd, J=3.7, 0.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H),4.47 (m, 1H), 4.07 (m, 1H), 3.84 (m, 2H), 3.40 (m, 2H), 3.13 (m, 2H),2.89 (m, 1H), 2.64 (m, 1H), 1.98 (m, 2H), 1.77-1.30 (m, 6H); MS (ESI(+))m/e 454 (M+H)⁺.

Example 8425-[1-(2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.9 Hz, 1H), 8.86 (s, 1H),8.47 (s, 1H), 7.83 (d, J=9.1 Hz, 1H), 7.64 (m, 2H), 6.96 (d, J=3.8 Hz,1H), 4.52 (d, J=5.8 Hz, 2H), 4.47 (m, 1H), 4.02 (m, 1H), 3.12 (m, 2H),2.88 (m, 1H), 2.63 (m, 1H), 1.99 (m, 2H), 1.43 (m, 2H), 1.00 (m, 6H); MS(ESI(+)) m/e 412 (M+H)⁺.

Example 8435-[1-(3-methylbutanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3-methylbutanoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.9 Hz, 1H), 8.86 (d,J=1.5 Hz, 1H), 8.47 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64 (m, 2H),6.95 (dd, J=3.7, 0.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H), 4.48 (m, 1H), 3.96(m, 1H), 3.10 (m, 2H), 2.63 (m, 1H), 2.21 (m, 2H), 1.98 (m, 3H), 1.43(m, 2H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 426 (M+H)⁺.

Example 8445-{1-[(2S)-2-methylbutanoyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (2S)-2-methylbutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.9 Hz,1H), 8.86 (d, J=1.5 Hz, 1H), 8.47 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H),7.64 (m, 2H), 6.95 (d, J⁼3.8 Hz, 1H), 4.52 (d, J=5.8 Hz, 2H), 4.49 (m,1H), 4.05 (m, 1H), 3.13 (m, 2H), 2.69 (m, 2H), 1.99 (m, 2H), 1.61-1.18(m, 4H), 0.98 (m, 3H), 0.82 (m, 3H); MS (ESI(+)) m/e 426 (M+H)⁺.

Example 8455-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (1-methylcyclopropyl)carboxylic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.9 Hz,1H), 8.86 (d, J=1.5 Hz, 1H), 8.47 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H),7.64 (m, 2H), 6.96 (dd, J=3.7, 0.9 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 4.33(m, 2H), 3.10 (m, 1H), 2.92 (m, 2H), 1.98 (m, 2H), 1.47 (m, 2H), 1.23(s, 3H), 0.80 (m, 2H), 0.53 (m, 2H); MS (ESI(+)) m/e 424 (M+H)⁺.

Example 846N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 3,3,3-trifluoropropanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t, J=5.9 Hz,1H), 8.86 (m, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.65 (m,2H), 6.95 (dd, J=3.7, 0.9 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 4.45 (m, 1H),3.90 (m, 1H), 3.66 (m, 2H), 3.13 (m, 2H), 2.70 (m, 1H), 1.97 (m, 2H),1.57 (m, 1H), 1.42 (m, 1H); MS (ESI(+)) m/e 452 (M+H)⁺.

Example 847N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 4,4,4-trifluorobutanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.8 Hz,1H), 8.86 (m, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64 (m,2H), 6.95 (dd, J=3.7, 0.8 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 4.47 (m, 1H),3.94 (m, 1H), 3.12 (m, 2H), 2.65 (m, 3H), 2.50 (m, 2H), 1.96 (m, 2H),1.57 (m, 1H), 1.41 (m, 1H); MS (ESI(+)) m/e 466 (M+H)⁺.

Example 8485-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (4,4-difluorocyclohexyl)carboxylic acidfor 4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.8Hz, 1H), 8.86 (m, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64(m, 2H), 6.96 (dd, J=3.7, 0.8 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 4.48 (m,1H), 4.06 (m, 1H), 3.13 (m, 2H), 2.82 (m, 1H), 2.65 (m, 1H), 2.10-1.80(m, 6H), 1.80-1.30 (m, 6H); MS (ESI(+)) m/e 488 (M+H)⁺.

Example 8495-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazlo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and tetrahydro-2H-pyran-4-ylcarboxylic acidfor 4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.9Hz, 1H), 8.86 (m, 1H), 8.48 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64(m, 2H), 6.95 (dd, J=3.7, 0.8 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 4.48 (m,1H), 4.06 (m, 1H), 3.84 (m, 2H), 3.38 (m, 2H), 3.12 (m, 2H), 2.89 (m,1H), 2.64 (m, 1H), 1.98 (m, 2H), 1.65-1.30 (m, 6H); MS (ESI(+)) m/e 454(M+H)⁺.

Example 8505-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 2-hydroxy-2-methylpropanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.8 Hz,1H), 8.86 (m, 1H), 8.47 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64 (m,2H), 6.95 (dd, J=3.7, 0.8 Hz, 1H), 5.39 (s, 1H), 5.00-4.30 (m, 2H), 4.53(d, J=5.8 Hz, 2H), 3.10 (m, 1H), 3.10-2.60 (m, 2H), 1.96 (m, 2H), 1.50(m, 2H), 1.32 (s, 6H); MS (ESI(+)) m/e 428 (M+H)⁺.

Example 8515-{1-[(1-methylpiperidin-4-yl)carbonyl]piperidin-4-yl}-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and (1-methylpiperidin-4-yl)carboxylic acidfor 4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t, J=5.8Hz, 1H), 8.85 (s, 1H), 8.47 (s, 1H), 7.83 (d, J=9.1 Hz, 1H), 7.64 (m,2H), 6.95 (d, J=3.8 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 4.48 (m, 1H), 4.00(m, 1H), 3.04 (m, 4H), 2.80-2.57 (m, 4H), 2.13 (s, 3H), 2.07-1.80 (m,4H), 1.81-0.93 (m, 4H); MS (ESI(+)) m/e 467 (M+H)⁺.

Example 8525-[1-(2-cyanobenzoyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and 2-cyanobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.02 (t, J=5.8 Hz, 1H), 8.86 (m,1H), 8.47 (s, 1H), 7.95 (m, 1H), 7.82 (m, 2H), 7.70-7.57 (m, 4H), 6.96(dd, J=3.7, 0.8 Hz, 1H), 4.61 (m, 1H), 4.52 (d, J=5.8 Hz, 2H), 3.35 (m,1H), 3.14 (m, 2H), 2.97 (m, 1H), 2.09 (m, 1H), 1.89 (m, 1H), 1.60 (m,2H); MS (ESI(+)) m/e 471 (M+H)⁺.

Example 8535-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor 3-methylbutan-1-amine and pyridin-2-ylcarboxylic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.03 (t, J=5.8 Hz,1H), 8.86 (m, 1H), 8.59 (m, 1H), 8.48 (s, 1H), 7.92 (td, J=7.7, 1.7 Hz,1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64 (m, 2H), 7.57 (dt, J=7.7, 1.1Hz, 1H), 7.47 (m, 1H), 6.97 (dd, J=3.7, 0.8 Hz, 1H), 4.58 (m, 1H), 4.53(d, J=5.8 Hz, 2H), 3.72 (m, 1H), 3.17 (m, 2H), 2.93 (m, 1H), 2.08 (m,1H), 1.91 (m, 1H), 1.58 (m, 2H); MS (ESI(+)) m/e 447 (M+H)⁺.

Example 8542-cyclopentyl-N-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}acetamide

The title compound was prepared as described in Example 1A, substitutingN-(4-aminophenyl)-2-cyclopentylacetamide for 3-methylbutan-1-amine and2-(imidazo[1,2-a]pyridin-6-yl)acetic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 10.12 (bs, 1H), 9.77 (bs, 1H), 8.47-8.44(m, 1H), 7.94 (s, 1H), 7.58-7.43 (m, 6H), 7.19 (dd, J=9.2, 1.7 Hz, 1H),3.64 (bs, 2H), 2.30-2.19 (m, 3H), 1.82-1.65 (m, 2H), 1.66-1.43 (m, 4H),1.26-1.08 (m, 2H); MS (ESI(+)) m/e 377 (M+H)⁺.

Example 855 tert-butyl4-{4-[(imidazo[1,2-b]pyridazin-6-ylmethyl)carbamoyl]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-b]pyridazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yl)benzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.15 (t, J=5.9 Hz, 1H), 8.24 (s,1H), 8.07 (d, J=9.3 Hz, 1H), 7.88-7.82 (m, 2H), 7.75 (d, J=1.2 Hz, 1H),7.41-7.34 (m, 2H), 7.20 (d, J=9.3 Hz, 1H), 4.63 (d, J=5.8 Hz, 2H),4.13-4.03 (m, 2H), 2.91-2.67 (m, 3H), 1.80-1.72 (m, 2H), 1.61-1.44 (m,2H), 1.42 (s, 9H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 8564-[(cyclopentylacetyl)amino]-N-(imidazo[1,2-b]pyridazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-b]pyridazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(2-cyclopentylacetamido)benzoic acid for 4-nitrobenzoic acid. ¹H NMR(400 MHz, methanol-d₄) δ ppm 8.38 (d, J=1.9 Hz, 1H), 8.28 (dd, J=9.4,0.7 Hz, 1H), 8.07 (d, J=1.9 Hz, 1H), 7.90-7.84 (m, 2H), 7.79-7.66 (m,3H), 4.91-4.79 (m, 2H), 2.43-2.25 (m, 3H), 1.92-1.78 (m, 2H), 1.79-1.50(m, 4H), 1.33-1.18 (m, 2H); MS (ESI(+)) m/e 378 (M+H)⁺.

Example 8575-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 857A methyl 5-(3-cyclopropylpropioloyl)thiophene-2-carboxylate

Methyl 5-(chlorocarbonyl)thiophene-2-carboxylate (500 mg, 2.443 mmol)was dissolved in triethylamine (5 mL) and the suspension was degassedwith nitrogen. Copper(I) iodide (40 mg, 0.210 mmol) andbistriphenylphosphine palladium chloride (40 mg, 0.057 mmol) were addedfollowed by ethynylcyclopropane (162 mg, 2.443 mmol). The mixture wasstirred overnight, diluted with methanol and concentrated to dryness.The crude material was partitioned between dichloromethane and water.The organic extracts were dried with sodium sulfate, filtered,concentrated and purified by normal phase chromatography to afford thetitle compound.

Example 857B methyl5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)thiophene-2-carboxylate

Methyl 5-(3-cyclopropylpropioloyl)thiophene-2-carboxylate (100 mg, 0.427mmol) was dissolved in N,N-dimethylformamide (2 mL), and the solutionwas cooled to 0° C. Benzylhydrazine hydrochloride (74.5 mg, 0.470 mmol)was added followed by potassium carbonate (77 mg, 0.555 mmol). Themixture was stirred at 0° C. until the ice bath melted and was stirredovernight at room temperature. The solution was partitioned betweenwater and ethyl acetate. The organic extract was dried with sodiumsulfate, filtered, concentrated and purified by normal phasechromatography to afford the title compound.

Example 857C5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)thiophene-2-carboxylic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)thiophene-2-carboxylatefor methyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 857D5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and5-(1-benzyl-3-cyclopropyl-1H-pyrazol-5-yl)thiophene-2-carboxylic acidfor 4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04 (t, J=5.9Hz, 1H), 8.49 (dd, J=7.0, 0.9 Hz, 1H), 7.91-7.87 (m, 1H), 7.74 (d, J=3.9Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.42-7.24 (m, 5H), 7.23-7.15 (m, 2H),6.84 (dd, J=7.0, 1.7 Hz, 1H), 6.38 (s, 1H), 5.44 (bs, 2H), 4.47 (d,J=5.9 Hz, 2H), 1.94-1.81 (m, 1H), 0.97-0.86 (m, 2H), 0.72-0.59 (m, 2H);MS (ESI(+)) m/e 454 (M+H)⁺.

Example 8585-[1-(2,2-dimethylpropyl)-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamideExample 858A5-bromo-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and5-bromothiophene-2-carboxylic acid for 4-nitrobenzoic acid.

Example 858B

The title compound was prepared as described in Example 51A,substituting1-neopentyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.10-8.99 (m, 2H),8.53 (d, J=1.3 Hz, 1H), 8.17 (d, J=0.9 Hz, 1H), 8.10 (d, J=0.5 Hz, 1H),7.82-7.78 (m, 2H), 7.76 (d, J=3.8 Hz, 1H), 7.23 (d, J=3.9 Hz, 1H), 4.54(d, J=5.7 Hz, 2H), 3.92 (s, 2H), 0.92 (s, 9H); MS (ESI(+)) m/e 395(M+H)⁺.

Example 8595-[1-(propan-2-ylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 682,substituting propane-2-sulfonyl chloride for benzenesulfonyl chlorideandN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.03 (t, J=5.8 Hz, 1H), 8.86 (d, J=1.5 Hz,1H), 8.48 (s, 1H), 7.83 (dd, J=9.1, 0.9 Hz, 1H), 7.64 (m, 2H), 6.97 (dd,J=3.7, 0.9 Hz, 1H), 4.53 (d, J=5.8 Hz, 2H), 3.71 (m, 2H), 3.25 (m, 1H),3.02 (m, 3H), 2.00 (m, 2H), 1.56 (m, 2H), 1.22 (d, J=6.8 Hz, 6H); MS(ESI(+)) m/e 448 (M+H)⁺.

Example 8605-[1-(phenylsulfonyl)piperidin-4-yl]-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 682,substitutingN-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)-5-(piperidin-4-yl)thiophene-2-carboxamidefor N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 9.01 (t, J=5.9 Hz, 1H), 8.85 (s, 1H), 8.47(s, 1H), 7.83 (d, J=9.1 Hz, 1H), 7.81-7.69 (m, 3H), 7.71-7.55 (m, 4H),6.90 (d, J=3.8 Hz, 1H), 4.51 (d, J=5.8 Hz, 2H), 3.73 (m, 2H), 2.84 (m,1H), 2.37 (m, 2H), 1.99 (m, 2H), 1.61 (m, 2H); MS (ESI(+)) m/e 482(M+H)⁺.

Example 861N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[(4-methyltetrahydro-2H-pyran-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-((4-methyltetrahydro-2H-pyran-4-yl)methyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.09-9.01 (m, 2H),8.53 (d, J=1.4 Hz, 1H), 8.18-8.15 (m, 1H), 8.13 (d, J=0.5 Hz, 1H),7.83-7.79 (m, 2H), 7.76 (d, J=3.9 Hz, 1H), 7.23 (d, J=3.9 Hz, 1H), 4.54(d, J=5.7 Hz, 2H), 4.04 (s, 2H), 3.68 (dt, J=11.4, 4.5 Hz, 2H), 3.51(ddd, J=11.8, 9.2, 2.9 Hz, 2H), 1.50 (ddd, J=13.4, 9.1, 4.1 Hz, 2H),1.33-1.18 (m, 2H), 0.96 (s, 3H); MS (ESI(+)) m/e 437 (M+H)⁺.

Example 862 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for3-methylbutan-1-amine and 2-(imidazo[1,2-a]pyridin-6-yl)acetic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.14 (s, 1H), 8.52(s, 1H), 8.01 (d, J=1.3 Hz, 1H), 7.65-7.58 (m, 2H), 7.54-7.47 (m, 2H),7.31 (dd, J=9.2, 1.7 Hz, 1H), 7.20-7.13 (m, 2H), 4.11-3.99 (m, 2H), 3.68(s, 2H), 2.89-2.54 (m, 3H), 1.76-1.66 (m, 2H), 1.53-1.32 (m, 11H); MS(ESI(+)) m/e 435 (M+H)⁺.

Example 863N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamideExample 863A2-(imidazo[1,2-a]pyridin-6-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-{4-[(imidazo[1,2-a]pyridin-6-ylacetyl)amino]phenyl}piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 863BN-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamide

The title compound was prepared as described in Example 1A, substituting2-(imidazo[1,2-a]pyridin-6-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide for3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, methanol-d₄) δ ppm 8.77 (s, 1H), 8.21 (d, J=2.2 Hz,1H), 8.03 (d, J=2.1 Hz, 1H), 8.01-7.94 (m, 1H), 7.93-7.87 (m, 1H),7.55-7.35 (m, 4H), 7.33-7.26 (m, 1H), 7.25-7.17 (m, 3H), 4.83-4.74 (m,1H), 3.91 (s, 2H), 3.68-3.58 (m, 1H), 3.30-3.18 (m, 1H), 3.02-2.78 (m,2H), 2.01-1.91 (m, 1H), 1.87-1.50 (m, 3H); MS (ESI(+)) m/e 457 (M+H)⁺.

Example 864N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(phenylsulfonyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 682,substitutingN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide forN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide. ¹H NMR(400 MHz, methanol-d₄) δ ppm 9.04-8.96 (m, 1H), 8.51 (s, 1H), 8.05 (s,1H), 7.85-7.79 (m, 5H), 7.73-7.66 (m, 1H), 7.67-7.59 (m, 2H), 7.35-7.28(m, 2H), 4.72-4.67 (m, 2H), 3.96-3.88 (m, 2H), 2.63-2.51 (m, 1H),2.48-2.37 (m, 2H), 1.93-1.85 (m, 2H), 1.86-1.72 (m, 2H); MS (ESI(+)) m/e476 (M+H)⁺.

Example 8652-(imidazo[1,2-a]pyridin-6-yl)-N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}acetamide

The title compound was prepared as described in Example 1A, substituting2-(imidazo[1,2-a]pyridin-6-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.77 (d, J=1.4 Hz, 1H), 8.21 (dd,J=2.2, 0.7 Hz, 1H), 8.03 (d, J=2.2 Hz, 1H), 8.01-7.94 (m, 1H), 7.93-7.87(m, 1H), 7.53-7.47 (m, 2H), 7.23-7.17 (m, 2H), 4.73-4.64 (m, 1H),4.21-4.13 (m, 1H), 3.91 (s, 2H), 3.27-3.14 (m, 1H), 2.99 (hept, J=6.7Hz, 1H), 2.88-2.74 (m, 1H), 2.76-2.63 (m, 1H), 1.96-1.81 (m, 2H),1.71-1.45 (m, 2H), 1.16-1.07 (m, 6H); MS (ESI(+)) m/e 405 (M+H)⁺.

Example 866N-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-6-yl)acetamide

The title compound was prepared as described in Example 1A, substituting2-(imidazo[1,2-a]pyridin-6-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide for3-methylbutan-1-amine and 2,4-difluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.77 (d, J=1.4 Hz, 1H),8.23-8.18 (m, 1H), 8.03 (d, J=2.2 Hz, 1H), 8.01-7.94 (m, 1H), 7.93-7.87(m, 1H), 7.54-7.42 (m, 3H), 7.25-7.19 (m, 2H), 7.13-7.05 (m, 2H),4.84-4.74 (m, 2H), 3.91 (s, 2H), 3.68-3.59 (m, 1H), 3.30-3.20 (m, 1H),3.02-2.79 (m, 1H), 2.00-1.91 (m, 1H), 1.88-1.52 (m, 3H); MS (ESI(+)) m/e475 (M+H)⁺.

Example 877N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}benzamideExample 877A methyl4-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)benzoate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(methoxycarbonyl)benzoic acid for 4-nitrobenzoic acid.

Example 877B 4-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)benzoic acid

The title compound was prepared as described in Example 4B, substitutingmethyl 4-((imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl)benzoate formethyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 877CN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(2-methylpropyl)pyrrolidin-1-yl]carbonyl}benzamide

The title compound was prepared as described in Example 1A, substituting2-isobutylpyrrolidine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.17 (t, J=5.9 Hz,1H), 8.49 (dd, J=6.9, 0.9 Hz, 1H), 7.95 (d, J=8.2 Hz, 2H), 7.89 (d,J=1.2 Hz, 1H), 7.56 (d, J=8.0 Hz, 2H), 7.52 (d, J=1.2 Hz, 1H), 7.40 (s,1H), 6.86 (dd, J=7.0, 1.7 Hz, 1H), 4.52 (d, J=5.9 Hz, 2H), 4.25-4.14 (m,1H), 3.58-3.51 (m, 1H), 3.51-3.38 (m, 1H), 2.09-1.53 (m, 5H), 1.33-1.17(m, 2H), 0.94 (d, J=6.4 Hz, 6H); MS (ESI(+)) m/e 405 (M+H)⁺.

Example 878N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]carbonyl}benzamide

The title compound was prepared as described in Example 1A, substituting(2R)-2-(methoxymethyl)pyrrolidine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.18 (t, J=4.8 Hz,1H), 8.49 (dd, J=7.0, 0.9 Hz, 1H), 7.95 (d, J=8.3 Hz, 2H), 7.88 (s, 1H),7.57 (d, J=7.7 Hz, 2H), 7.52 (d, J=1.2 Hz, 1H), 7.40 (s, 1H), 6.86 (dd,J=7.0, 1.6 Hz, 1H), 4.52 (d, J=5.9 Hz, 2H), 3.62-2.88 (br m, 8H),2.05-1.64 (br m, 4H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 881N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(phenylsulfonyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-7-ylmethanamine for 3-methylbutan-1-amine and4-(phenylsulfonyl)benzoic acid for 4-nitrobenzoic acid. ¹H NMR (400 MHz,DMSO-d₆) δ ppm 9.53 (t, J=5.9 Hz, 1H), 8.83 (d, J=6.9 Hz, 1H), 8.30 (d,J=2.1 Hz, 1H), 8.16-8.07 (m, 5H), 8.03-7.97 (m, 2H), 7.80-7.61 (m, 4H),7.46 (dd, J=6.9, 1.6 Hz, 1H), 4.68 (d, J=5.8 Hz, 2H); MS (ESI(+)) m/e392 (M+H)⁺.

Example 8824-(phenylsulfonyl)-N-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substituting[1,2,4]triazolo[1,5-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amineand 4-(phenylsulfonyl)benzoic acid for 4-nitrobenzoic acid. ¹H NMR (400MHz, DMSO-d₆) δ ppm 9.32 (t, J=5.8 Hz, 1H), 8.92-8.87 (m, 1H), 8.49-8.46(m, 1H), 8.07 (m, 4H), 8.01-7.95 (m, 2H), 7.85-7.78 (m, 1H), 7.75-7.67(m, 1H), 7.68-7.60 (m, 3H), 4.57 (d, J=5.7 Hz, 2H); MS (ESI(+)) m/e 393(M+H)⁺.

Example 889N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}furan-2-carboxamideExample 889A tert-butyl4-(2-(4-(5-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)furan-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)furan-2-carboxamide for4-bromoaniline.

Example 889BN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}furan-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(2-(4-(5-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)furan-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, 2H), 9.28 (t, J=6.1 Hz, 1H),8.87 (d, J=6.7 Hz, 1H), 8.33 (s, 2H), 8.15 (d, J=2.1 Hz, 1H), 8.00 (s,1H), 7.82 (s, 1H), 7.49 (dd, J=7.0, 1.5 Hz, 1H), 7.26 (d, J=3.5 Hz, 1H),6.72 (d, J=3.5 Hz, 1H), 4.73-4.59 (m, 4H), 3.66-3.56 (m, 2H), 3.41 (d,J=11.4 Hz, 8H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 8925-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 857,substituting methylhydrazine for benzylhydrazine in Example 857B. ¹H NMR(300 MHz, DMSO-d₆) δ 9.04 (t, J=6.0 Hz, 1H), 8.49 (dd, J=7.0, 0.9 Hz,1H), 7.89 (s, 1H), 7.73 (d, J=3.9 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.40(s, 1H), 7.30 (d, J=3.8 Hz, 1H), 6.85 (dd, J=7.0, 1.7 Hz, 1H), 6.32 (s,1H), 4.47 (d, J=5.9 Hz, 2H), 3.84 (s, 3H), 1.97-1.84 (m, 1H), 1.04-0.89(m, 2H), 0.75-0.63 (m, 2H); MS (ESI(+)) m/e 378 (M+H)⁺.

Example 8935-[3-cyclopropyl-1-(2-methoxyethyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 857,substituting (2-methoxyethyl)hydrazine for benzylhydrazine in Example857B. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.04 (t, J=6.0 Hz, 1H), 8.49 (dd,J=7.0, 1.0 Hz, 1H), 7.89 (s, 1H), 7.73 (d, J=3.9 Hz, 1H), 7.52 (d, J=1.2Hz, 1H), 7.40 (s, 1H), 7.31 (d, J=3.8 Hz, 1H), 6.85 (dd, J=7.0, 1.7 Hz,1H), 6.31 (s, 1H), 4.47 (d, J=5.9 Hz, 2H), 4.33 (t, J=5.5 Hz, 2H), 3.73(t, J=5.5 Hz, 2H), 3.24 (s, 3H), 2.00-1.87 (m, 1H), 1.01-0.92 (m, 2H),0.72-0.63 (m, 2H); MS (ESI(+)) m/e 422 (M+H)⁺.

Example 894N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamideExample 894A tert-butyl4-(2-(4-(5-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)thiophen-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline.

Example 894BN-(imidazo[1,2-a]pyrazin-6-ylmethyl)-5-{1-[2-(piperazin-1-yl)ethyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(2-(4-(5-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)thiophen-2-yl)-1H-pyrazol-1-yl)ethyl)piperazine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.52 (s, 2H), 9.28-9.17 (m, 2H), 8.68(d, J=1.2 Hz, 1H), 8.36-8.30 (m, 1H), 8.27 (d, J=0.4 Hz, 1H), 8.05 (d,J=1.4 Hz, 1H), 7.91 (d, J=0.5 Hz, 1H), 7.81 (d, J=3.9 Hz, 1H), 7.27 (d,J=3.9 Hz, 1H), 4.71-4.48 (m, 2H), 4.07 (s, 8H), 3.37 (s, 4H); MS(ESI(+)) m/e 437 (M+H)⁺.

Example 897N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(phenylsulfonyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(phenylsulfonyl)benzoic acid for 4-nitrobenzoic acid. ¹H NMR (400 MHz,DMSO-d₆) δ ppm 9.38 (t, J=5.8 Hz, 1H), 9.11 (s, 1H), 8.61-8.57 (m, 1H),8.18 (s, 1H), 8.16-8.03 (m, 4H), 8.04-7.97 (m, 2H), 7.93-7.89 (m, 1H),7.76-7.68 (m, 1H), 7.70-7.61 (m, 2H), 4.60 (d, J=5.7 Hz, 2H); MS(ESI(+)) m/e 393 (M+H)⁺.

Example 898N-(imidazo[1,2-a]pyridin-6-ylmethyl)-4-(phenylsulfonyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyridin-6-ylmethanamine for 3-methylbutan-1-amine and4-(phenylsulfonyl)benzoic acid for 4-nitrobenzoic acid. ¹H NMR (400 MHz,DMSO-d₆) δ ppm 9.47 (t, J=5.8 Hz, 1H), 8.82 (s, 1H), 8.35-8.30 (m, 1H),8.19-8.14 (m, 1H), 8.12-8.08 (m, 4H), 8.05-7.88 (m, 4H), 7.76-7.68 (m,1H), 7.68-7.60 (m, 2H), 4.61 (d, J=5.8 Hz, 2H); MS (ESI(+)) m/e 392(M+H)⁺.

Example 899N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting1-isobutyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.24 (t, J=5.9 Hz,1H), 8.51 (dd, J=7.0, 0.7 Hz, 1H), 7.90 (d, J=0.8 Hz, 1H), 7.87 (d,J=3.9 Hz, 1H), 7.57-7.49 (m, 2H), 7.43 (s, 1H), 7.39 (d, J=3.9 Hz, 1H),6.87 (dd, J=7.0, 1.6 Hz, 1H), 6.56 (d, J=1.9 Hz, 1H), 4.51 (d, J=5.9 Hz,2H), 4.08 (d, J=7.4 Hz, 2H), 2.09 (dp, J=13.8, 6.9 Hz, 1H), 0.80 (d,J=6.7 Hz, 6H); MS (ESI(+)) m/e 380 (M+H)⁺.

Example 900 tert-butyl4-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for3-methylbutan-1-amine and 2-(imidazo[1,2-a]pyridin-7-yl)acetic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.16 (s, 1H), 8.55(d, J=6.9 Hz, 1H), 7.97 (s, 1H), 7.65-7.53 (m, 2H), 7.53-7.47 (m, 2H),7.20-7.13 (m, 2H), 7.01-6.95 (m, 1H), 4.09-4.00 (m, 2H), 3.72 (s, 2H),2.87-2.55 (m, 3H), 1.76-1.67 (m, 2H), 1.50-1.35 (m, 11H); MS (ESI(+))m/e 435 (M+H)⁺.

Example 901N-[(3-chloroimidazo[1,2-a]pyrazin-6-yl)methyl]-4-[(cyclopentylacetyl)amino]benzamide

The title compound was prepared as described in Example 396,substituting4-(2-cyclopentylacetamido)-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamidefor4-(3-imidazo[1,2-a]pyridin-6-ylureido)-N-((tetrahydro-2H-pyran-2-yl)methyl)benzamide.¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.07 (s, 1H), 9.09 (s, 1H), 8.95 (t,J=5.7 Hz, 1H), 8.28 (s, 1H), 7.95 (s, 1H), 7.87-7.81 (m, 2H), 7.69-7.63(m, 2H), 4.61 (d, J=5.6 Hz, 2H), 2.38-2.12 (m, 3H), 1.80-1.64 (m, 2H),1.66-1.40 (m, 4H), 1.25-1.09 (m, 2H); MS (ESI(+)) m/e 412 (M+H)⁺.

Example 902N-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamideExample 902A2-(imidazo[1,2-a]pyridin-7-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-{4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 902BN-{4-[1-(2,4-difluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide

The title compound was prepared as described in Example 1A, substituting2-(imidazo[1,2-a]pyridin-7-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide for3-methylbutan-1-amine and 2,4-difluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.29 (s, 1H), 8.84 (d, J=6.9 Hz,1H), 8.31 (d, J=1.9 Hz, 1H), 8.14 (d, J=2.1 Hz, 1H), 7.89 (s, 1H),7.56-7.47 (m, 3H), 7.47-7.40 (m, 1H), 7.42-7.31 (m, 1H), 7.23-7.15 (m,3H), 4.68-4.60 (m, 1H), 3.95 (bs, 2H), 3.58-3.44 (m, 1H), 3.26-3.09 (m,1H), 2.94-2.70 (m, 2H), 1.94-1.81 (m, 1H), 1.79-1.40 (m, 3H); MS(ESI(+)) m/e 475 (M+H)⁺.

Example 9032-(imidazo[1,2-a]pyridin-7-yl)-N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}acetamide

The title compound was prepared as described in Example 1A, substituting2-(imidazo[1,2-a]pyridin-7-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide for3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, DMSO-d₆) δ ppm 10.28 (s, 1H), 8.84 (d, J=6.9 Hz, 1H),8.34-8.28 (m, 1H), 8.18-8.14 (m, 1H), 7.89 (s, 1H), 7.55-7.43 (m, 3H),7.22-7.16 (m, 2H), 4.60-4.50 (m, 1H), 4.09-4.00 (m, 1H), 3.96 (s, 2H),3.18-3.01 (m, 1H), 2.96-2.82 (m, 1H), 2.79-2.67 (m, 1H), 2.63-2.50 (m,1H), 1.87-1.70 (m, 2H), 1.57-1.30 (m, 2H), 1.07-0.93 (m, 6H); MS(ESI(+)) m/e 405 (M+H)⁺.

Example 9041-[(3-chloroimidazo[1,2-a]pyridin-7-yl)methyl]-3-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}urea

The title compound was prepared as described in Example 396,substituting1-(imidazo[1,2-a]pyridin-7-ylmethyl)-3-(4-(1-isobutyrylpiperidin-4-yl)phenyl)ureafor4-(3-imidazo[1,2-a]pyridin-6-ylureido)-N-((tetrahydro-2H-pyran-2-yl)methyl)benzamide.¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.31 (bs, 1H), 8.24 (d, J=7.0 Hz, 1H),7.58 (s, 1H), 7.46 (s, 1H), 7.35-7.29 (m, 2H), 7.12-7.02 (m, 3H),6.62-6.55 (m, 1H), 4.38 (d, J=6.0 Hz, 2H), 4.36-4.19 (m, 2H), 2.93-2.62(m, 4H), 1.85-1.77 (m, 2H), 1.53-1.37 (m, 2H), 1.03 (d, J=6.7 Hz, 6H);MS (ESI(+)) m/e 454 (M+H)⁺.

Example 905N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamide

The title compound was prepared as described in Example 1A, substituting2-(imidazo[1,2-a]pyridin-7-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide for3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, methanol-d₄) δ ppm 8.75 (d, J=7.0 Hz, 1H), 8.18 (d,J=2.2 Hz, 1H), 8.00 (d, J=2.2 Hz, 1H), 7.89 (s, 1H), 7.56-7.35 (m, 5H),7.33-7.25 (m, 1H), 7.25-7.17 (m, 3H), 4.83-4.74 (m, 1H), 3.99 (s, 2H),3.68-3.59 (m, 1H), 3.31-3.18 (m, 1H), 3.03-2.76 (m, 2H), 2.00-1.92 (m,1H), 1.87-1.51 (m, 3H); MS (ESI(+)) m/e 457 (M+H)⁺.

Example 906N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-methyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 857,substituting 4-methylpent-1-yne for ethynylcyclopropane in Example 857Aand methylhydrazine for benzylhydrazine in Example 857B. ¹H NMR (400MHz, DMSO-d₆) δ ppm 9.05 (t, J=5.9 Hz, 1H), 8.49 (dd, J=6.9, 0.9 Hz,1H), 7.89 (s, 1H), 7.74 (d, J=3.9 Hz, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.40(s, 1H), 7.35 (d, J=3.8 Hz, 1H), 6.85 (dd, J=6.9, 1.7 Hz, 1H), 6.46 (s,1H), 4.48 (d, J=5.9 Hz, 2H), 3.75 (s, 3H), 2.54-2.51 (m, 2H), 1.96-1.84(m, 1H), 0.94 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 394 (M+H)⁺.

Example 9075-[1-benzyl-3-(2-methylpropyl)-1H-pyrazol-5-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 857,substituting 4-methylpent-1-yne for ethynylcyclopropane in Example 857A.¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.05 (t, J=5.8 Hz, 1H), 8.49 (dd, J=7.0,0.9 Hz, 1H), 7.89 (s, 1H), 7.76 (d, J=3.9 Hz, 1H), 7.52 (d, J=1.2 Hz,1H), 7.42-7.38 (m, 2H), 7.37-7.23 (m, 3H), 7.17-7.11 (m, 2H), 6.85 (dd,J=7.0, 1.7 Hz, 1H), 6.56 (s, 1H), 5.35 (bs, 2H), 4.48 (d, J=5.9 Hz, 2H),2.49-2.45 (m, 2H), 1.87-1.74 (m, 1H), 0.87 (d, J=6.6 Hz, 6H); MS(ESI(+)) m/e 470 (M+H)⁺.

Example 9084-[(cyclopentylacetyl)amino]-2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(2-cyclopentylacetamido)-2-fluorobenzoic acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.27 (s, 1H), 9.13 (s, 1H), 8.73-8.65(m, 1H), 8.59-8.56 (m, 1H), 8.24 (s, 1H), 7.94-7.91 (m, 1H), 7.75-7.67(m, 2H), 7.34 (dd, J=8.5, 1.9 Hz, 1H), 4.59 (d, J=5.8 Hz, 2H), 2.37-2.32(m, 2H), 2.32-2.16 (m, 1H), 1.82-1.68 (m, 2H), 1.67-1.44 (m, 4H),1.26-1.10 (m, 2H); MS (ESI(+)) m/e 396 (M+H)⁺.

Example 909N-(2,5-difluorobenzyl)-N′-(imidazo[1,2-a]pyridin-7-ylmethyl)benzene-1,4-dicarboxamide

The title compound was prepared as described in Example 1A, substituting2,5-difluorobenzyl amine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.42 (t, J=5.9 Hz,1H), 9.20 (t, J=5.8 Hz, 1H), 8.83 (d, J=6.9 Hz, 1H), 8.29 (d, J=2.0 Hz,1H), 8.10 (d, J=2.0 Hz, 1H), 8.04-8.00 (m, 4H), 7.78 (s, 1H), 7.45 (dd,J=6.9, 1.6 Hz, 1H), 7.32-7.12 (m, 3H), 4.69 (d, J=5.8 Hz, 2H), 4.52 (d,J=5.7 Hz, 2H); MS (ESI(+)) m/e 421 (M+H)⁺.

Example 910N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{[2-(propan-2-yl)pyrrolidin-1-yl]carbonyl}benzamide

The title compound was prepared as described in Example 1A, substituting(propan-2-yl)pyrrolidine for 3-methylbutan-1-amine and4-(imidazo[1,2-a]pyridin-7-ylmethylcarbamoyl)benzoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.44-9.36 (m, 1H),8.86 (d, J=6.9 Hz, 1H), 8.31 (d, J=2.1 Hz, 1H), 8.14 (d, J=2.1 Hz, 1H),8.01-7.95 (m, 2H), 7.80 (s, 1H), 7.65-7.59 (m, 2H), 7.49 (d, J=7.6 Hz,1H), 4.69 (d, J=5.8 Hz, 2H), 4.15-4.05 (m, 1H), 3.47-3.19 (m, 2H),2.39-2.26 (m, 1H), 1.96-1.57 (m, 4H), 0.93-0.85 (m, 6H); MS (ESI(+)) m/e391 (M+H)⁺.

Example 911N-{4-[5-(2,2-dimethylpropyl)-1,3,4-oxadiazol-2-yl]phenyl}-2-(imidazo[1,2-a]pyridin-7-yl)acetamideExample 911A N′-(3,3-dimethylbutanoyl)-4-nitrobenzohydrazide

A suspension of 4-nitrobenzohydrazide (0.500 g, 2.76 mmol), and4-methylmorpholine (0.455 ml, 4.14 mmol) were stirred in dichloromethane(20 ml). 3,3-Dimethylbutanoyl chloride (0.422 ml, 3.04 mmol) was addedand the reaction mixture was stirred for 2 hours. Normal phasechromatography of the crude reaction mixture gave the title compound.

Example 911B 2-neopentyl-5-(4-nitrophenyl)-1,3,4-oxadiazole

A mixture of N′-(3,3-dimethylbutanoyl)-4-nitrobenzohydrazide (0.556 g,1.991 mmol) and methyl N-(triethylammoniumsulfonyl)carbamate (0.572 g,2.389 mmol) in tetrahydrofuran (10 ml) was heated to 120° C. in amicrowave (Biotage Initiator) for 45 minutes. The crude reaction mixturewas concentrated and purified by normal phase chromatography to give thetitle compound.

Example 911C 4-(5-neopentyl-1,3,4-oxadiazol-2-yl)aniline

The title compound was prepared as described in Example 1B, substituting2-neopentyl-5-(4-nitrophenyl)-1,3,4-oxadiazole for tert-butyl4-(4-(1-(benzyloxycarbonyl)azetidine-3-carboxamido)phenoxy)piperidine-1-carboxylate.

Example 911DN-{4-[5-(2,2-dimethylpropyl)-1,3,4-oxadiazol-2-yl]phenyl}-1-(pyridazin-3-yl)azetidine-3-carboxamide

The title compound was prepared as described in Example 1A, substituting4-(5-neopentyl-1,3,4-oxadiazol-2-yl)aniline for tert-butyl4-(4-aminophenoxy)piperidine-1-carboxylate and2-(imidazo[1,2-a]pyridin-7-yl)acetic acid for1-(benzyloxycarbonyl)azetidine-3-carboxylic acid. ¹H NMR (400 MHz,DMSO-d₆) δ ppm 10.55 (s, 1H), 8.49 (d, J=7.0 Hz, 1H), 7.96-7.89 (m, 3H),7.86-7.79 (m, 2H), 7.53 (d, J=1.1 Hz, 1H), 7.49 (s, 1H), 6.88 (dd,J=7.0, 1.6 Hz, 1H), 3.77 (s, 2H), 2.82 (s, 2H), 1.02 (s, 9H); MS(ESI(+)) m/e 390 (M+H)⁺.

Example 912 tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylateExample 912A tert-butyl4-(4-amino-3-fluorophenyl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 4-bromo-2-fluoroaniline for 4-bromoaniline.

Example 912B tert-butyl4-(4-amino-3-fluorophenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1B, substitutingtert-butyl4-(4-amino-3-fluorophenyl)-5,6-dihydropyridine-1(2H)-carboxylate forN-isopentyl-4-nitrobenzamide.

Example 912C tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1C, substitutingtert-butyl 4-(4-amino-3-fluorophenyl)piperidine-1-carboxylate for4-amino-N-isopentylbenzamide and imidazo[1,2-a]pyridin-7-ylmethanaminefor imidazo[1,2-a]pyridin-6-amine. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.49(d, J=7.0 Hz, 1H), 8.37 (d, J=2.3 Hz, 1H), 7.97 (t, J=8.5 Hz, 1H), 7.88(s, 1H), 7.52 (d, J=1.2 Hz, 1H), 7.39 (s, 1H), 7.12-7.04 (m, 2H),7.00-6.94 (m, 1H), 6.82 (dd, J=7.0, 1.6 Hz, 1H), 4.35 (d, J=5.9 Hz, 2H),4.10-4.01 (m, 2H), 2.89-2.56 (m, 3H), 1.77-1.68 (m, 2H), 1.41 (s, 11H);MS (ESI(+)) m/e 468 (M+H)⁺.

Example 958N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrrolidin-1-ylcarbonyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 1068,substituting pyrrolidine-1-carbonyl chloride for piperidine-1-carbonylchloride. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.28-9.21 (m, 1H), 8.85 (d,J=7.0 Hz, 1H), 8.31 (d, J=2.1 Hz, 1H), 8.13 (d, J=2.1 Hz, 1H), 7.91-7.85(m, 2H), 7.77 (s, 1H), 7.47 (dd, J=7.0, 1.6 Hz, 1H), 7.43-7.36 (m, 2H),4.67 (d, J=5.8 Hz, 2H), 3.83-3.75 (m, 2H), 3.35-3.23 (m, 4H), 2.85-2.72(m, 3H), 1.81-1.69 (m, 6H), 1.71-1.53 (m, 2H); MS (ESI(+)) m/e 432(M+H)⁺.

Example 1067 tert-butyl4-{3-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingtert-butyl 4-(4-amino-3-fluorophenyl)piperidine-1-carboxylate for3-methylbutan-1-amine and 2-(imidazo[1,2-a]pyridin-7-yl)acetic acidhydrochloride for 4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm9.97 (s, 1H), 8.58 (d, J=6.9 Hz, 1H), 8.00 (s, 1H), 7.77-7.67 (m, 2H),7.58 (d, J=1.4 Hz, 1H), 7.15 (dd, J=12.2, 1.9 Hz, 1H), 7.06-6.99 (m,2H), 4.10-4.01 (m, 2H), 3.82 (bs, 2H), 2.94-2.58 (m, 3H), 1.78-1.69 (m,2H), 1.53-1.36 (m, 11H); MS (ESI(+)) m/e 453 (M+H)⁺.

Example 1068N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]benzamide

A solution of piperidine-1-carbonyl chloride (0.033 g, 0.224 mmol) inN-methyl-2-pyrrolidinone (1 mL) was treated withN-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-(piperidin-4-yl)benzamide (0.05g, 0.150 mmol) and triethylamine (0.042 ml, 0.299 mmol) and the reactionmixture was stirred at room temperature for 18 hours. The mixture waspurified by reverse-phase HPLC to give the title compound. ¹H NMR (400MHz, DMSO-d₆) δ ppm 9.24 (t, J=5.9 Hz, 1H), 8.84 (d, J=7.0 Hz, 1H), 8.30(d, J=2.1 Hz, 1H), 8.13 (d, J=2.1 Hz, 1H), 7.91-7.84 (m, 2H), 7.76 (s,1H), 7.50-7.44 (m, 1H), 7.42-7.36 (m, 2H), 4.67 (d, J=5.8 Hz, 2H),3.71-3.62 (m, 2H), 3.16-3.10 (m, 4H), 2.89-2.68 (m, 3H), 1.81-1.72 (m,2H), 1.68-1.44 (m, 8H); MS (ESI(+)) m/e 446 (M+H)⁺.

Example 10691-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureaExample 1069A1-(2-fluoro-4-(piperidin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(3-fluoro-4-{[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]amino}phenyl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 1069B1-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-3-(imidazo[1,2-a]pyridin-7-ylmethyl)urea

The title compound was prepared as described in Example 1A, substituting1-(2-fluoro-4-(piperidin-4-yl)phenyl)-3-(imidazo[1,2-a]pyridin-7-ylmethyl)ureafor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.73 (d, J=7.0 Hz, 1H), 8.16 (d, J=2.1Hz, 1H), 7.99-7.95 (m, 1H), 7.85-7.77 (m, 2H), 7.50-7.39 (m, 6H),7.11-6.99 (m, 2H), 4.84-4.72 (m, 1H), 4.60 (bs, 2H), 3.93-3.73 (m, 1H),3.29-3.15 (m, 1H), 3.00-2.76 (m, 2H), 2.03-1.84 (m, 1H), 1.83-1.53 (m,3H); MS (ESI(+)) m/e 472 (M+H)⁺.

TABLE 25 The following Examples were prepared essentially as describedin Example 1069, substituting an appropriate carboxylic acid in Example1069B. Ex Name MS 1070 1-{4-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]-2-(ESI(+)) fluorophenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 452 ylmethyl)urea(M + H)⁺ 1071 1-{4-[1-(3,3-dimethylbutanoyl)piperidin-4-yl]-2- (ESI(+))fluorophenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 466 ylmethyl)urea (M + H)⁺1072 1-{2-fluoro-4-[1-(4-methylpentanoyl)piperidin-4- (ESI(+))yl]phenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 466 ylmethyl)urea (M + H)⁺1073 1-(2-fluoro-4-{1-[(2S)-2-methylbutanoyl]piperidin-4- (ESI(+))yl}phenyl)-3-(imidazo[1,2-a]pyridin-7- m/e 452 ylmethyl)urea (M + H)⁺1074 1-{2-fluoro-4-[1-(tetrahydro-2H-pyran-4-ylcarbon- (ESI(+))yl)piperidin-4-yl]phenyl}-3-(imidazo[1,2- m/e 480a]pyridin-7-ylmethyl)urea (M + H)⁺ 10751-{2-fluoro-4-[1-(pyridin-2-ylcarbonyl)piperidin-4- (ESI(+))yl]phenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 473 ylmethyl)urea (M + H)⁺1076 1-{4-[1-(2-cyanobenzoyl)piperidin-4-yl]-2- (ESI(+))fluorophenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 497 ylmethyl)urea (M + H)⁺1078 1-{2-fluoro-4-[1-(2-methylpropanoyl)piperidin-4- (ESI(+))yl]phenyl}-3-(imidazo[1,2-a]pyridin-7- m/e 438 ylmethyl)urea (M + H)⁺

Example 10774-{4-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]phenyl}-N,N-dimethylpiperidine-1-carboxamide

The title compound was prepared as described in Example 1068,substituting N,N-dimethylamine-1-carbonyl chloride forpiperidine-1-carbonyl chloride. ¹H NMR (400 MHz, methanol-d₄) δ ppm 8.75(d, J=7.0 Hz, 1H), 8.19-8.15 (m, 1H), 8.01-7.97 (m, 1H), 7.89-7.83 (m,2H), 7.80 (s, 1H), 7.51-7.46 (m, 1H), 7.44-7.38 (m, 2H), 4.77 (s, 2H),3.85-3.76 (m, 2H), 2.98-2.77 (m, 9H), 1.90-1.81 (m, 2H), 1.81-1.66 (m,2H); MS (ESI(+)) m/e 406 (M+H)⁺.

Example 10794-[(cyclopentylacetyl)amino]-N-[(7-fluoroimidazo[1,2-a]pyridin-6-yl)methyl]benzamide

The title compound was prepared as described in Example 1A, substituting(7-fluoroimidazo[1,2-a]pyridin-6-yl)methanamine for3-methylbutan-1-amine and 4-(2-cyclopentylacetamido)benzoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 10.08 (s, 1H), 8.87(t, J=5.5 Hz, 1H), 8.56 (d, J=7.3 Hz, 1H), 7.96 (s, 1H), 7.88-7.82 (m,2H), 7.71-7.64 (m, 2H), 7.52 (d, J=1.2 Hz, 1H), 7.46-7.39 (m, 1H), 4.49(d, J=5.5 Hz, 2H), 2.36-2.30 (m, 2H), 2.31-2.15 (m, 1H), 1.81-1.68 (m,2H), 1.68-1.43 (m, 4H), 1.26-1.10 (m, 2H); MS (ESI(+)) m/e 395 (M+H)⁺.

Example 1080N-[(7-fluoroimidazo[1,2-a]pyridin-6-yl)methyl]-5-[1-(2-methylpropyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

The title compound was prepared as described in Example 1A, substituting(7-fluoroimidazo[1,2-a]pyridin-6-yl)methanamine for3-methylbutan-1-amine and5-(1-isobutyl-1H-pyrazol-4-yl)thiophene-2-carboxylic acid for4-nitrobenzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.93 (t, J=5.5 Hz,1H), 8.58 (d, J=7.7 Hz, 1H), 8.14 (d, J=0.8 Hz, 1H), 7.98 (s, 1H), 7.80(d, J=0.8 Hz, 1H), 7.73 (d, J=3.8 Hz, 1H), 7.53 (d, J=1.3 Hz, 1H), 7.44(d, J=11.0 Hz, 1H), 7.21 (d, J=3.8 Hz, 1H), 4.48 (d, J=5.5 Hz, 2H), 3.92(d, J=7.2 Hz, 2H), 2.21-2.05 (m, 1H), 0.85 (d, J=6.7 Hz, 6H); MS(ESI(+)) m/e 398 (M+H)⁺.

Example 1081N-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-2-(imidazo[1,2-a]pyridin-7-yl)acetamideExample 1081AN-(2-fluoro-4-(piperidin-4-yl)phenyl)-2-(imidazo[1,2-a]pyridin-7-yl)acetamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-{3-fluoro-4-[(imidazo[1,2-a]pyridin-7-ylacetyl)amino]phenyl}piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 1081BN-[4-(1-benzoylpiperidin-4-yl)-2-fluorophenyl]-2-(imidazo[1,2-a]pyridin-7-yl)acetamide

The title compound was prepared as described in Example 1A, substitutingN-(2-fluoro-4-(piperidin-4-yl)phenyl)-2-(imidazo[1,2-a]pyridin-7-yl)acetamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, methanol-d₄) δ ppm 8.75 (dd, J=6.9, 0.9 Hz, 1H), 8.19 (dd,J=2.2, 0.8 Hz, 1H), 8.00 (d, J=2.2 Hz, 1H), 7.91 (s, 1H), 7.78 (t, J=8.2Hz, 1H), 7.53-7.38 (m, 6H), 7.16-7.04 (m, 2H), 4.83-4.69 (m, 1H), 4.06(s, 2H), 3.91-3.79 (m, 1H), 3.30-3.14 (m, 1H), 3.03-2.81 (m, 2H),2.07-1.54 (m, 4H); MS (ESI(+)) m/e 457 (M+H)⁺.

Example 1154N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(pyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide

The title compound was prepared as described in Example 51A,substituting4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridin-1(2H)-yl)pyrimidine for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 4-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO d₆) δ ppm 9.32 (t, J=5.9 Hz, 1H),8.90-8.80 (m, 2H), 8.38 (dd, J=7.5, 1.2 Hz, 1H), 8.31 (d, J=2.0 Hz, 1H),8.14 (d, J=2.1 Hz, 1H), 7.95 (d, J=8.5 Hz, 2H), 7.80 (s, 1H), 7.63 (d,J=8.4 Hz, 2H), 7.47 (dd, J=7.0, 1.5 Hz, 1H), 7.32-7.18 (m, 1H),6.48-6.40 (m, 1H), 4.68 (d, J=5.8 Hz, 2H), 4.57-4.47 (m, 2H), 4.19-4.04(m, 2H), 2.74-2.64 (m, 2H); MS (ESI(+)) m/e 411 (M+H)⁺.

Example 1155N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-[1-(2-methylpyrimidin-4-yl)-1,2,3,6-tetrahydropyridin-4-yl]benzamide

The title compound was prepared as described in Example 51A,substituting2-methyl-4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridin-1(2H)-yl)pyrimidine for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 4-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.07-8.95 (m, 1H), 8.78(dd, J=7.0, 0.5 Hz, 1H), 8.28-8.16 (m, 2H), 8.00 (d, J=2.0 Hz, 1H),7.97-7.87 (m, 2H), 7.80-7.74 (m, 1H), 7.63-7.54 (m, 2H), 7.40 (dd,J=7.0, 1.5 Hz, 1H), 7.04 (d, J=7.4 Hz, 1H), 6.41-6.31 (m, 1H), 4.66 (m,2H), 4.47 (m, 2H), 4.10 (t, J=5.8 Hz, 2H), 2.77-2.64 (m, 2H), 2.55 (s,3H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 1156N-(imidazo[1,2-a]pyridin-7-ylmethyl)-4-{1-[6-(trifluoromethyl)pyrimidin-4-yl]-1,2,3,6-tetrahydropyridin-4-yl}benzamide

The title compound was prepared as described in Example 51A,substituting4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridin-1(2H)-yl)-6-(trifluoromethyl)pyrimidine for1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 4-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)benzamide for4-bromoaniline. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.30 (t, J=5.9 Hz, 1H),8.84 (d, J=6.9 Hz, 1H), 8.68 (s, 1H), 8.29 (d, J=2.0 Hz, 1H), 8.11 (d,J=2.1 Hz, 1H), 7.99-7.89 (m, 2H), 7.77 (s, 1H), 7.72-7.58 (m, 2H), 7.45(dd, J=7.0, 1.5 Hz, 1H), 7.38-7.20 (m, 1H), 6.43 (m, 1H), 4.67 (d, J=5.8Hz, 2H), 4.53-4.31 (m, 2H), 4.13-3.92 (m, 2H), 2.70-2.62 (m, 2H); MS(ESI(+)) m/e 479 (M+H)⁺.

Example 11575-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamideExample 1157A5-bromo-3,7-dimethyltricyclo[3.3.1.1^(3,7)]decane-1-carboxylic acid

In a 50 mL round-bottomed flask, bromine (3 mL) was cooled to 0 OC andiron (0.56 g) was added. The mixture was stirred at 0 OC for 30 minutes.3,5-Dimethyladamantane-1-carboxylic acid (0.5 g) was added. The mixturewas stirred at room temperature overnight. After adding ice and 6Naqueous HCl (10 mL), ethyl acetate (20 mL), and saturated aqueous sodiumsulfite were added. The aqueous layer was extracted twice with ethylacetate. The combined organic layers were washed with saturated sodiumsulfite and dried over sodium sulfate. After filtration and removal ofthe solvent, the product was used directly in the next step.

Example 1157B5-bromo-3,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-ylmethanol

To a solution of5-bromo-3,7-dimethyltricyclo[3.3.1.1^(3,7)]decane-1-carboxylic acid(4.57 g, 15.9 mmol) in tetrahydrofuran (10 mL) was added boranetetrahydrofuran complex (50 mL, 1 M in THF) dropwise and the mixture wasstirred at room temperature for 14 hours. The reaction mixture wasquenched with methanol, concentrated and purified by normal phasechromatography to provide the title compound.

Example 1157C1-(5-bromo-3,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-yl)-1H-pyrazole

To a solution of the5-bromo-3,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-ylmethanol (8.0 g, 29.3mmol) in toluene (60 mL) was added 1H-pyrazole (1.55 g, 22.7 mmol) andcyanomethylenetributylphosphorane (2.0 g, 29.3 mmol) under nitrogen.After the addition, the mixture was stirred at 90° C. overnight. Thereaction mixture was then concentrated, and the residue was purified bynormal phase chromatography to give the title compound.

Example 1157D2-{[3,5-dimethyl-7-(1H-pyrazol-1-ylmethyl)tricyclo[3.3.1.1^(3,7)]dec-1-yl]oxy}ethanol

To a solution of1-(5-bromo-3,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-yl)-1H-pyrazole (4.5g) in ethane-1,2-diol (12 mL) was added triethylamine (3 mL) undernitrogen. The mixture was heated to 150 OC in a Biotage Initiatormicrowave reactor for 45 minutes. The mixture was poured over water andextracted with ethyl acetate. The combined organic layers were washedwith water and brine, dried with sodium sulfate, filtered andconcentrated. The residue was purified by normal phase chromatography togive the title compound.

Example 1157E2-({3,5-dimethyl-7-[(5-methyl-1H-pyrazol-1-yl)methyl]tricyclo[3.3.1.1^(3,7)]dec-1-yl}oxy)ethanol

To a cold (−78° C.) solution of the2-{[3,5-dimethyl-7-(1H-pyrazol-1-ylmethyl)tricyclo[3.3.1.1^(3,7)]dec-1-yl]oxy}ethanol(3.69 g) in tetrahydrofuran (50 mL) was added n-butyllithium (20 mL, 2.5M in hexane) under nitrogen. The mixture was stirred at −78° C. for 1.5hours. Iodomethane (10 mL) was added by syringe, and the mixture wasstirred for an additional 3 hours. The reaction mixture was thenquenched by the addition of aqueous ammonium chloride solution andextracted with ethyl acetate. The combined organic layers were washedwith water and brine, dried with sodium sulfate, filtered andconcentrated. The residue was purified by normal phase chromatography togive the title compound.

Example 1157F1-({3,5-dimethyl-7-[2-(hydroxy)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-4-iodo-5-methyl-1H-pyrazole

To a solution of the2-({3,5-dimethyl-7-[(5-methyl-1H-pyrazol-1-yl)methyl]tricyclo[3.3.1.1^(3,7)]dec-1-yl}oxy)ethanol(3.5 g, 11 mmol) in N,N-dimethylformamide (30 ml) was addedN-iodosuccinimide (3.2 g, 14.22 mmol). The mixture was stirred at roomtemperature for 1.5 hours. The reaction mixture was then diluted withethyl acetate and washed with aqueous sodium thiosulfate, water andbrine. After drying over anhydrous sodium sulfate, the mixture wasfiltered and concentrated. The residue was purified by normal phasechromatography to give the title compound.

Example 1157G2-({3-[(4-iodo-5-methyl-1H-pyrazol-1-yl)methyl]-5,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-yl}oxy)ethylmethanesulfonate

To a cold (0° C.) solution of1-({3,5-dimethyl-7-[2-(hydroxy)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-4-iodo-5-methyl-1H-pyrazole(2.1 g) in methylene chloride (30 mL) was added triethylamine (1.42 g)followed by methanesulfonyl chloride (0.542 g). The mixture was stirredat room temperature for 1.5 hours and then was diluted with ethylacetate. The layers were separated, and the organic layer was washedwith water and brine, dried with sodium sulfate, filtered andconcentrated to give the title compound, which was used in the next stepwithout further purification.

Example 1157H1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-4-iodo-5-methyl-1H-pyrazole

A solution of2-({3-[(4-iodo-5-methyl-1H-pyrazol-1-yl)methyl]-5,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-yl}oxy)ethylmethanesulfonate (2.5 g) in 2 M methylamine in methanol (15 mL) washeated to 100° C. for 20 minutes in a Biotage Initiator microwavereactor. The reaction mixture was concentrated, and the residue wasdiluted with ethyl acetate. The organic layer was washed with saturatedaqueous sodium bicarbonate solution, water and brine. The organic layerwas dried with sodium sulfate, filtered and concentrated to give thetitle compound which was used in the next reaction without furtherpurification.

Example 1157Itert-butyl[2-({3-[(4-iodo-5-methyl-1H-pyrazol-1-yl)methyl]-5,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-yl}oxy)ethyl]methylcarbamate

To a solution of1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-4-iodo-5-methyl-1H-pyrazole(2.2 g) in tetrahydrofuran (30 mL) was added Boc-anhydride (1.26 g) anda catalytic amount of 4-dimethylaminopyridine. The mixture was stirredat room temperature for 1.5 hours and diluted with ethyl acetate. Thesolution was washed with saturated aqueous sodium bicarbonate, water andbrine. The organic layer was dried with sodium sulfate, filtered andconcentrated. The residue was purified by normal phase chromatography togive the title compound

Example 1157J tert-butyl{2-[(3,5-dimethyl-7-{[5-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}tricyclo[3.3.1.1^(3,7)]dec-1-yl)oxy]ethyl}methylcarbamate

To a solution oftert-butyl[2-({3-[(4-iodo-5-methyl-1H-pyrazol-1-yl)methyl]-5,7-dimethyltricyclo[3.3.1.1^(3,7)]dec-1-yl}oxy)ethyl]methylcarbamate(2.8 g, 5.02 mmol) in dioxane (40 ml) was addedbis(benzonitrile)palladium(II) chloride (96 mg, 0.251 mmol), S-Phos (206mg, 0.502 mmol), and pinacolborane (2 mL) followed by triethylamine (2.5mL, 5.25 mmol) under nitrogen. The mixture was stirred at refluxovernight. The reaction mixture was then diluted with ethyl acetate andwashed with water and brine. After drying (anhydrous sodium sulfate),the solution was filtered and concentrated and the residue was purifiedby normal phase chromatographyto give the title compound.

Example 1157K5-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

The title compound was prepared as described in Example 51A,substituting tert-butyl{2-[(3,5-dimethyl-7-{[5-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}tricyclo[3.3.1.1^(3,7)]dec-1-yl)oxy]ethyl}methylcarbamatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand 5-bromo-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamidefor 4-bromoaniline followed by deprotection as described in Example 28A.¹H NMR (400 MHz, DMSO-d₆) δ 9.50 (t, J=5.9 Hz, 1H), 8.88 (d, J=7.0 Hz,1H), 8.76-8.64 (m, 2H), 8.34 (d, J=2.0 Hz, 1H), 8.16 (d, J=2.1 Hz, 1H),7.93 (d, J=3.9 Hz, 1H), 7.83 (s, 1H), 7.76 (s, 1H), 7.49 (dd, J=7.0, 1.3Hz, 1H), 7.23 (d, J=3.9 Hz, 1H), 4.65 (d, J=5.8 Hz, 2H), 3.92 (s, 2H),3.63-3.55 (m, 2H), 3.04-2.91 (m, 2H), 2.51 (dd, J=6.0, 3.7 Hz, 3H), 2.45(s, 3H), 1.42 (s, 2H), 1.31 (dd, J=27.3, 11.4 Hz, 4H), 1.16 (q, J=12.5Hz, 4H), 1.07-0.99 (m, 2H), 0.87 (s, 6H); MS (ESI(+)) m/e 587 (M+H)⁺.

Example 11582-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamideExample 1158A tert-butyl4-(3-fluoro-4-(methoxycarbonyl)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 51A,substituting tert-butyl4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylatefor1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleand methyl 4-bromo-2-fluorobenzoate for 4-bromoaniline.

Example 1158B tert-butyl4-(3-fluoro-4-(methoxycarbonyl)phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1B, substitutingtert-butyl 4-(3-fluoro-4-(methoxycarbonyl)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate for N-isopentyl-4-nitrobenzamide.

Example 1158C 4-(1-(tert-butoxycarbonyl)piperidin-4-yl)-2-fluorobenzoicacid

The title compound was prepared as described in Example 4B, substitutingtert-butyl4-(3-fluoro-4-(methoxycarbonyl)phenyl)piperidine-1-carboxylate formethyl 4-(3-imidazo[1,2-a]pyridin-6-ylureido)benzoate.

Example 1158D tert-butyl4-(3-fluoro-4-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingimidazo[1,2-a]pyrazin-6-ylmethanamine for 3-methylbutan-1-amine and4-(1-(tert-butoxycarbonyl)piperidin-4-yl)-2-fluorobenzoic acid for4-nitrobenzoic acid.

Example 1158E2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(3-fluoro-4-((imidazo[1,2-a]pyrazin-6-ylmethyl)carbamoyl)phenyl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 1158F2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-{1-[(1-methylcyclopropyl)carbonyl]piperidin-4-yl}benzamide

The title compound was prepared as described in Example 1A, substituting2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamidefor 3-methylbutan-1-amine and 1-methylcyclopropanecarboxylic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, METHANOL-d₄) δ ppm 9.27 (s, 1H),8.72 (s, 1H), 8.28 (d, J=1.5 Hz, 1H), 8.11 (d, J=1.6 Hz, 1H), 7.78 (t,J=7.9 Hz, 1H), 7.27-7.11 (m, 2H), 4.79 (s, 2H), 4.63-4.51 (m, 2H),3.23-2.72 (m, 3H), 1.99-1.88 (m, 2H), 1.71-1.54 (m, 2H), 1.33 (s, 3H),1.02-0.83 (m, 2H), 0.73-0.55 (m, 2H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 11594-(1-benzoylpiperidin-4-yl)-2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)benzamide

The title compound was prepared as described in Example 1A, substituting2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamidefor 3-methylbutan-1-amine and benzoic acid for 4-nitrobenzoic acid. ¹HNMR (400 MHz, METHANOL-d₄) δ ppm 9.28-9.20 (m, 1H), 8.74-8.65 (m, 1H),8.30-8.21 (m, 1H), 8.13-8.05 (m, 1H), 7.79 (t, J=7.9 Hz, 1H), 7.51-7.40(m, 5H), 7.29-7.14 (m, 2H), 4.85-4.72 (m, 3H), 3.94-3.76 (m, 1H),3.30-3.14 (m, 1H), 3.05-2.86 (m, 2H), 2.07-1.60 (m, 4H); MS (ESI(+)) m/e458 (M+H)⁺.

Example 11602-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(2-methylpropanoyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 1A, substituting2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamidefor 3-methylbutan-1-amine and isobutyric acid for 4-nitrobenzoic acid.¹H NMR (400 MHz, METHANOL-d₄) δ ppm 9.26 (s, 1H), 8.75-8.66 (m, 1H),8.31-8.22 (m, 1H), 8.14-8.06 (m, 1H), 7.78 (t, J=8.0 Hz, 1H), 7.27-7.10(m, 2H), 4.79 (s, 2H), 4.75-4.66 (m, 1H), 4.26-4.14 (m, 1H), 3.29-3.15(m, 1H), 3.09-2.86 (m, 2H), 2.79-2.61 (m, 1H), 2.05-1.85 (m, 2H),1.74-1.48 (m, 2H), 1.18-1.05 (m, 6H); MS (ESI(+)) m/e 424 (M+H)⁺.

Example 11612-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]benzamide

The title compound was prepared as described in Example 1A, substituting2-fluoro-N-(imidazo[1,2-a]pyrazin-6-ylmethyl)-4-(piperidin-4-yl)benzamidefor 3-methylbutan-1-amine and 3,3,3-trifluoropropanoic acid for4-nitrobenzoic acid. ¹H NMR (400 MHz, METHANOL-d₄) δ ppm 9.24 (s, 1H),8.74-8.65 (m, 1H), 8.30-8.21 (m, 1H), 8.13-8.04 (m, 1H), 7.78 (t, J=7.9Hz, 1H), 7.27-7.10 (m, 2H), 4.78 (s, 2H), 4.72-4.64 (m, 1H), 4.14-4.00(m, 1H), 3.63-3.45 (m, 2H), 3.30-3.21 (m, 1H), 3.03-2.86 (m, 1H), 2.77(m, 1H), 1.98-1.86 (m, 2H), 1.65 (m, 2H); MS (ESI(+)) m/e 464 (M+H)⁺.

Example 1162N-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)acetamideExample 1162A tert-butyl4-(4-(2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)acetamido)phenyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1A, substitutingtert-butyl 4-(4-aminophenyl)piperidine-1-carboxylate for3-methylbutan-1-amine and 2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)aceticacid hydrochloride for 4-nitrobenzoic acid.

Example 1162B2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)-N-(4-(piperidin-4-yl)phenyl)acetamide

The title compound was prepared as described in Example 28A,substituting tert-butyl4-(4-(2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)acetamido)phenyl)piperidine-1-carboxylatefor tert-butyl4-(4-(3-imidazo[1,2-a]pyridin-6-ylureido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 1162CN-{4-[1-(2-fluorobenzoyl)piperidin-4-yl]phenyl}-2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)acetamide

The title compound was prepared as described in Example 1A, substituting2-([1,2,4]triazolo[4,3-a]pyridin-6-yl)-N-(4-(piperidin-4-yl)phenyl)acetamidefor 3-methylbutan-1-amine and 2-fluorobenzoic acid for 4-nitrobenzoicacid. ¹H NMR (400 MHz, METHANOL-d₄) δ ppm 10.28-10.20 (m, 1H), 9.30 (s,1H), 8.54 (s, 1H), 7.85-7.74 (m, 1H), 7.63-7.46 (m, 4H), 7.41-7.31 (m,3H), 7.31-7.20 (m, 2H), 4.77-4.65 (m, 1H), 3.75 (s, 2H), 3.56-3.46 (m,1H), 3.30-3.15 (m, 1H), 2.99-2.75 (m, 2H), 1.97-1.86 (m, 1H), 1.81-1.49(m, 3H); MS (ESI(+)) m/e 458 (M+H)⁺.

Example 1163N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-({4-methyl-1-[2-(piperazin-1-yl)ethyl]piperidin-4-yl}methyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide

A solution ofN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide(0.100 g, 0.197 mmol) in N,N-dimethylformamide (2 ml) was addedtert-butyl 4-(2-bromoethyl)piperazine-1-carboxylate (0.058 g, 0.197mmol) followed by N,N-diisopropylethylamine (0.138 ml, 0.788 mmol) andthe reaction was stirred overnight. The reaction mixture was purifieddirectly using normal phase chromatography and the resulting materialwas treated with HCl in dioxane (4M) for 2 hours then concentrated togive the title compound as a hydrochloride salt. ¹H NMR (500 MHz,DMSO-d₆) δ 14.64 (s, 1H), 10.40 (s, 1H), 9.72 (s, 1H), 9.54 (t, J=6.0Hz, 1H), 8.89 (d, J=6.9 Hz, 1H), 8.34 (d, J=1.8 Hz, 1H), 8.22 (s, 1H),8.16 (d, J=2.1 Hz, 1H), 7.91 (d, J=3.9 Hz, 1H), 7.87 (s, 1H), 7.83 (s,1H), 7.50 (dd, J=7.0, 1.4 Hz, 1H), 7.28 (d, J=3.8 Hz, 1H), 4.64 (d,J=5.8 Hz, 2H), 4.23-3.54 (m, 10H), 3.35 (d, J=38.3 Hz, 8H), 1.72 (d,J=77.7 Hz, 4H), 0.98 (s, 3H); MS (ESI(+)) m/e 547 (M+H)⁺.

Example 1164S-(2-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-2-oxoethyl)-L-cysteine

A suspension ofN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide(0.100 g, 0.197 mmol) and 4-methylmorpholine (0.108 ml, 0.985 mmol) inN,N-diisopropylethylamine (0.5 ml) was added to 2,5-dioxopyrrolidin-1-yl2-bromoacetate (0.056 g, 0.236 mmol) in N,N-diisopropylethylamine (0.5ml) and stirred at room temperature. After 1 hour,(R)-2-amino-3-mercaptopropanoic acid (0.119 g, 0.985 mmol) as a solutionin water (1 ml) was added. After stirring an additional 1 hour, a fewdrops of TFA were added to form a homogeneous solution which waspurified by revere phase chromatography. The product containing peakswere lyophilized to give the title compound. ¹H NMR (400 MHz, DMSO-d₆) δ9.30 (t, J=6.0 Hz, 1H), 8.86 (d, J=7.0 Hz, 1H), 8.44 (bs, 2H), 8.32 (d,J=2.0 Hz, 1H), 8.18-8.11 (m, 2H), 7.86-7.77 (m, 3H), 7.46 (dd, J=7.0,1.5 Hz, 1H), 7.27 (dd, J=3.7, 1.8 Hz, 1H), 4.65 (d, J=5.8 Hz, 2H),4.21-4.13 (m, 1H), 4.13-4.02 (m, 2H), 4.02-3.92 (m, 1H), 3.87-3.57 (m,3H), 3.42-3.29 (m, 1H), 3.29-3.18 (m, 1H), 3.10 (dd, J=14.6, 4.7 Hz,1H), 2.98 (dd, J=14.6, 7.6 Hz, 1H), 1.60-1.18 (m, 4H), 0.96 (s, 3H); MS(ESI(+)) m/e 596 (M+H)⁺.

Example 11655-(1-{[1-(15-amino-4,7,10,13-tetraoxapentadecan-1-oyl)-4-methylpiperidin-4-yl]methyl}-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide

A suspension ofN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide(0.139 g, 0.274 mmol),2,2-dimethyl-4-oxo-3,8,11,14,17-pentaoxa-5-azaicosan-20-oic acid (0.100g, 0.274 mmol),2-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)-1,1,3,3-tetramethylisouroniumhexafluorophosphate(V) (0.104 g, 0.274 mmol) and 4-methylmorpholine(0.105 ml, 0.958 mmol) was stirred at room temperature for 3 hours. Thereaction mixture was purified directly by normal phase chromatographyand the resulting material was treated with HCl/dioxane (4 M) thenconcentrated to give the title compound as a hydrochloride salt. ¹H NMR(400 MHz, DMSO-d₆) δ 14.71 (s, 1H), 9.58 (t, J=6.0 Hz, 1H), 8.89 (d,J=7.0 Hz, 1H), 8.35 (d, J=1.9 Hz, 1H), 8.16 (d, J=2.1 Hz, 2H), 8.06 (s,3H), 7.92 (d, J=3.9 Hz, 1H), 7.83 (s, 2H), 7.50 (dd, J=7.0, 1.2 Hz, 1H),7.26 (d, J=3.8 Hz, 1H), 4.64 (d, J=5.8 Hz, 2H), 4.05 (s, 2H), 3.80 (dd,J=11.8, 6.8 Hz, 2H), 3.66-3.58 (m, 4H), 3.55 (dd, J=9.2, 4.4 Hz, 4H),3.50 (t, J=7.5 Hz, 8H), 3.37-3.26 (m, 1H), 3.23-3.13 (m, 1H), 2.99-2.90(m, 2H), 2.55 (t, J=6.6 Hz, 2H), 1.53-1.19 (m, 4H), 0.95 (s, 3H); MS(ESI(+)) m/e 682 (M+H)⁺.

Example 1166S-{2-[(3-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-3-oxopropyl)amino]-2-oxoethyl}-L-cysteine

A suspension ofN-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-{1-[(4-methylpiperidin-4-yl)methyl]-1H-pyrazol-4-yl}thiophene-2-carboxamide(0.050 g, 0.099 mmol) and 4-methylmorpholine (0.054 ml, 0.493 mmol) inN,N-diisopropylethylamine (0.5 ml) was added to 2,5-dioxopyrrolidin-1-yl3-(2-bromoacetamido)propanoate (0.036 g, 0.118 mmol) inN,N-diisopropylethylamine (0.5 ml) and the mixture was stirred at roomtemperature. After 1 hour, (R)-2-amino-3-mercaptopropanoic acid (0.060g, 0.493 mmol) as a solution in water (1 ml) was added. After 1 hour, afew drops of TFA were added to form a homogeneous solution and themixture was purified by chromatography to give the title compound. ¹HNMR (400 MHz, DMSO-d₆) δ 9.28 (t, J=5.9 Hz, 1H), 8.85 (d, J=7.0 Hz, 1H),8.47 (s, 2H), 8.30 (d, J=1.9 Hz, 1H), 8.21 (t, J=5.6 Hz, 1H), 8.17-8.09(m, 2H), 7.84 (s, 1H), 7.81-7.74 (m, 2H), 7.44 (dd, J=7.0, 1.1 Hz, 1H),7.27 (d, J=3.8 Hz, 1H), 4.65 (d, J=5.8 Hz, 2H), 4.20 (dd, J=7.5, 4.3 Hz,1H), 4.06 (s, 2H), 3.90-3.78 (m, 2H), 3.35-2.94 (m, 8H), 2.59-2.41 (m,2H), 1.57-1.19 (m, 4H), 0.95 (s, 3H); MS (ESI(+)) m/e 667 (M+H)⁺.

1-10. (canceled)
 11. A method of treating inflammatory and tissue repairdisorders; particularly rheumatoid arthritis, inflammatory boweldisease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia in apatient, said method comprising administering to the patient atherapeutically effective amount of a compound or a therapeuticallyacceptable salt thereof, selected from the group consisting of:5-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-({4-methyl-1-[2-(piperazin-1-yl)ethyl]piperidin-4-yl}methyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;S-(2-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-2-oxoethyl)-L-cysteine;5-(1-{[1-(15-amino-4,7,10,13-tetraoxapentadecan-1-oyl)-4-methylpiperidin-4-yl]methyl}-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;andS-{2-[(3-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-3-oxopropyl)amino]-2-oxoethyl}-L-cysteine.12. A method of treating inflammatory and tissue repair disorders;particularly rheumatoid arthritis, inflammatory bowel disease, asthmaand COPD (chronic obstructive pulmonary disease), osteoarthritis,osteoporosis and fibrotic diseases; dermatosis, including psoriasis,atopic dermatitis and ultra-violet induced skin damage; autoimmunediseases including systemic lupus erythematosis, multiple sclerosis,psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection,Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes,glomerulonephritis, cancer, particularly wherein the cancer is selectedfrom breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder,pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia,inflammation associated with infection and certain viral infections,including Acquired Immune Deficiency Syndrome (AIDS), adult respiratorydistress syndrome, and ataxia telengiectasia or spleen cancer in apatient, said method comprising administering to the patienttherapeutically effective amount of the compound or a therapeuticallyacceptable salt thereof, selected from the group consisting of:5-[1-({3,5-dimethyl-7-[2-(methylamino)ethoxy]tricyclo[3.3.1.1^(3,7)]dec-1-yl}methyl)-5-methyl-1H-pyrazol-4-yl]-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;N-(imidazo[1,2-a]pyridin-7-ylmethyl)-5-[1-({4-methyl-[2-(piperazin-1-yl)ethyl]piperidin-4-yl}methyl)-1H-pyrazol-4-yl]thiophene-2-carboxamide;S-(2-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-2-oxoethyl)-L-cysteine;5-(1-{[1-(15-amino-4,7,10,13-tetraoxapentadecan-1-oyl)-4-methylpiperidin-4-yl]methyl}-1H-pyrazol-4-yl)-N-(imidazo[1,2-a]pyridin-7-ylmethyl)thiophene-2-carboxamide;andS-{2-[(3-{4-[(4-{5-[(imidazo[1,2-a]pyridin-7-ylmethyl)carbamoyl]thiophen-2-yl}-1H-pyrazol-1-yl)methyl]-4-methylpiperidin-1-yl}-3-oxopropyl)amino]-2-oxoethyl}-1-cysteine;and a therapeutically effective amount of one additional therapeuticagent or more than one additional therapeutic agent.